| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Selisistat - EX 527 | Axon 1956
CAS [49843-98-3]
MF C13H13ClN2OMW 248.71
Purity:
99%
Soluble in DMSO
Description
Potent and selective deacetylase sirtin 1 (SIRT1) inhibitor; a useful tool for studying the relationship between SIRT1 and cell regulation; a potential agent the treatment of Huntington’s Disease (HD)
References
Certificates
Categories
Extra info
AD Napper et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J. Med. Chem. 2005, 48, 8045-8054.
JC Milne et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007, 450(7170), 712-716.
JM Solomon et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006, 26(1), 28-38.
Y Zhang et al. Deacetylation of cortactin by SIRT1 promotes cell migration. Oncogene. 2009, 28(3), 445-60.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
DNA-damage Response
EC 3.5.1.98
SIRT
Potent and selective SIRT1 inhibitor
Chemical name
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Parent CAS No.
[49843-98-3]
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Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| SRT 1720 tetrahydrochloride | Axon 1875
CAS [1001645-58-4]
MF C25H23N7OS.4HClMW 615.41
Purity:
99%
Soluble in water and DMSO
Description
A small-molecule activator of the sirtuin subtype SIRT1; 1000x more potent than resveratrol. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function
References
Certificates
Categories
Extra info
JC Milne et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature 2007, 450(7170), 712–7160.
H Dai et al. SIRT1 activation by small molecules - kinetic and biophysical evidence for direct interaction of enzyme and activator. J. Biol. Chem. 2010, 285(43), 32695–32703.
E Callaway. GlaxoSmithKline strikes back over anti-ageing pills: Drugs do work as thought, says pharmaceutical giant. Nature 2010-08-16.
RK Minor et al. SRT1720 improves survival and healthspan of obese mice. Scientific Reports 2011, 1, 70.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
Endocrinology
DNA-damage Response
EC 3.5.1.98
SIRT
Activator of the sirtuin subtype SIRT1
Chemical name
N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide tetrahydrochloride
Parent CAS No.
[925434-55-5]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| ML 323 | Axon 2309
CAS [1572414-83-5]
MF C23H24N6MW 384.48
Purity:
100%
Soluble in DMSO
Description
Selective, reversible and highly potent inhibitor of the USP1–UAF1 deubiquitinase complex that links deubiquitination to DNA damage responses (IC50 values of 76 nM in a ubiquitin-rhodamine (Ub-Rho) assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively). ML323 effectively sensitized cisplatin-resistant NSCLC H596 cells and U2OS osteosarcoma cells to cisplatin since it simultaneously targets two major DNA damage response pathways (TLS and FA) by inhibiting a common deubiquitinase.
KEYWORDS: ML 323 | USP1-UAF1 inhibitor | ML323 |CAS[1572414-83-5] | Ubiquitin peptides | Deubiquitinase | Inhibitor | DNA damage | cisplatin-resistant | TLS | FA | | axonmedchem |
| MG 132 | Axon 1869
CAS [133407-82-6]
MF C26H41N3O5MW 475.62
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Specific, potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM). MG132 inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 also activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis.
References
Certificates
Categories
Extra info
D Banerjee and A Liefshitz. Potential of the proteasomal inhibitor MG-132 as an anticancer agent, alone and in combination. Anticancer Res. 2001, 21(6A), 3941-3947.
VJ Palombella et al. The ubiquitin-proteasome pathway is required for processing the NF-kappa B1 precursor protein and the activation of NF-kappa B. Cell. 1994, 78(5), 773-785.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
MAPK (JNK)
Proteasome 26S
NF-κB
Ubiquitin
EC 3.4
Inhibitor of 26S proteasome
Chemical name
benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate
Parent CAS No.
[133407-82-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| NSC 687852 - b-AP15 | Axon 2228
CAS [1009817-63-3]
MF C22H17N3O6MW 419.39
Purity:
98%
Soluble in DMSO
Description
Inhibitor of two 19S regulatory-particle–associated deubiquitinases (DUBs), ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14) showing tumor growth inhibition in vivo. NSC 687852 shows IC50 values of 0.5 μM and 2.1 μM in cathepsin-dependent caspase-cleavage and in purified 19S proteasome Ub-AMC cleavage assays respectively.NSC 687852 induced tumor cell apoptosis that was insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2. UNC 687852 does not inhibit the non proteasomeal DUBs UCHL-1/3, USP-2/7/8 and BAP1.
References
Certificates
Categories
Extra info
P. D'Arcy et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat. Med. 2011, 17, 1636-1640.
M. Berndtsson et al. Induction of the lysosomal apoptosis pathway by inhibitors of the ubiquitin-proteasome system. Int. J. Cancer. 2009, 124, 1463-1469.
H.N. Pati et al. Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells. Eur. J. Med. Chem. 2008, 43, 1-7.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Inhibitor of 19S regulatory-particle–associated deubiquitinases (DUBs: UCHL5 and USP14)
Chemical name
(3E,5E)-1-acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one
Parent CAS No.
[1009817-63-3]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| P 22077 | Axon 1906
CAS [1247819-59-5]
MF C12H7F2NO3S2MW 315.32
Purity:
99%
Soluble in DMSO
Description
Small molecule inhibitor of deubiquitinase (DUB), specific on ubiquitin-specific protease 7 (USP7) and the closely related USP47; Inhibits USP7-mediated p53 deubiquitination
References
Certificates
Categories
Extra info
M Altun et al. Activity-Based Chemical Proteomics Accelerates Inhibitor Development for Deubiquitylating Enzymes. Chem. Biol. 2011, 18, 1401–1412.
X Tian et al. Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev. Technol. 2011, 9(2), 165-173.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Inhibitor of deubiquitinase USP7 and USP47
Chemical name
1-(5-(2,4-difluorophenylthio)-4-nitrothiophen-2-yl)ethanone
Parent CAS No.
[1247819-59-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Eeyarestatin I - ES1 | ERAD inhibitor 1 | p97 inhibitor 1 | Axon 1798
CAS [412960-54-4]
MF C27H25Cl2N7O7MW 630.44
Purity:
98%
Soluble in DMSO
Description
Potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination
References
Certificates
Categories
Extra info
BC Cross et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J. Cell Sci. 2009, 122(Pt 23), 4393-4400.
MO Aletrari et al. Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One. 2011, 6(7), e22713.
Q Wang et al. Inhibition of p97-dependent Protein Degradation by Eeyarestatin I. J. Biol. Chem. 2008, 283, 7445-7454.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Inhibitor of endoplasmic reticulum associated protein degradation (ERAD)
Chemical name
3-(4-chlorophenyl)-1-(3-(4-chlorophenyl)-5,5-dimethyl-1-(2-((E)-2-((E)-3-(5-nitrofuran-2-yl)allylidene)hydrazinyl)-2-oxoethyl)-2-oxoimidazolidin-4-yl)-1-hydroxyurea
Parent CAS No.
[412960-54-4]
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Size
Unit Price
Stock
2 mg
€80.00
In Stock | | axonmedchem |
| WP 1130 - Degrasyn | Axon 1779
CAS [856243-80-6]
MF C19H18BrN3OMW 384.27
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Small molecule inhibitor of deubiquitinase (DUB)
References
Certificates
Categories
Extra info
V Kapuria et al. A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination. Cell Signal. 2011, 23(12), 2076-2085.
V Kapuria et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010, 70(22), 9265-9276.
LV Pham et al. Degrasyn Potentiates the Antitumor Effects of Bortezomib in Mantle Cell Lymphoma Cells In vitro and In vivo: Therapeutic Implications. Mol Cancer Ther July 2010 9; 2026.
GA Bartholomeusz et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007, 109(8), 3470-3478.
GA Bartholomeusz et al. Degrasyn activates proteasomal-dependent degradation of c-Myc. Cancer Res. 2007, 67(8), 3912-3918.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Deubiquitinase Inhibitor
Chemical name
(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
Parent CAS No.
[856243-80-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MLN 8237 - Alisertib | Axon 2003
CAS [1028486-01-2]
MF C27H20ClFN4O4MW 518.92
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Second generation, orally bioavailable, potent and highly selective aurora A inhibitor
References
Certificates
Categories
Extra info
DA Sloane et al. Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237. ACS Chem. Biol. 2010, 5(6), 563-576.
G Görgün et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma. Blood. 2010, 115(25), 5202-5213.
M Tomita, N Mori. Aurora A selective inhibitor MLN8237 suppresses the growth and survival of HTLV-1-infected T-cells in vitro. Cancer Sci. 2010, 101(5), 1204-1211.
MG Manfredi et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays. Clin. Cancer Res. 2011, 17(24), 7614-7624.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Second generation selective Aurora A inhibitor
Chemical name
4-(9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[e]pyrimido[5,4-c]azepin-2-ylamino)-2-methoxybenzoic acid
Parent CAS No.
[1028486-01-2]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| MK 5108 - VX 689 | Axon 1961
CAS [1010085-13-8]
MF C22H21ClFN3O3SMW 461.94
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Highly potent and selective inhibitor of Aurora A kinase (AurA); MK5108 exhibits marked effects on the growth of tumor cells in vitro and in vivo; also enhances the antitumoractivity of Docetaxel without exacerbrating the toxicity in vivo
References
Certificates
Categories
Extra info
T Shimomura et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol. Cancer Ther. 2010, 9(1), 157-166.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Inhibitor of Aurora A kinase
Chemical name
(1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexanecarboxylic acid
Parent CAS No.
[1010085-13-8]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| MLN 0905 | Axon 1910
CAS [1228960-69-7]
MF C24H25F3N6SMW 486.56
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, orally available and selective polo-like kinase (PLK) 1 inhibitor
References
Certificates
Categories
Extra info
MO Duffey et al. Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905). J. Med. Chem. 2012, 55 (1), 197-208.
JQ Shi et al. MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol. Cancer Ther. 2012, 11(9), 2045-2053.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.11.21
PLK
PLK1 inhibitor
Chemical name
2-(5-(3-(dimethylamino)propyl)-2-methylpyridin-3-ylamino)-9-(trifluoromethyl)-5H-benzo[b]pyrimido[4,5-d]azepine-6(7H)-thione
Parent CAS No.
[1228960-69-7]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| P 005091 - P 5091 | Axon 2011
CAS [882257-11-6]
MF C12H7Cl2NO3S2MW 348.22
Purity:
99%
Soluble in DMSO
Description
Selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) and the closely related USP47; inhibits USP7-mediated p53 deubiquitination; enhances the degradation of the USP7 substrate HDM2 in tumor cells; induces apoptosis in MM cells resistant to conventional and bortezomib (Axon 1810) therapies
References
Certificates
Categories
Extra info
B Nicholson, KGS Kumar. The multifaceted roles of USP7: new therapeutic opportunities. Cell Biochem. Biophys. 2011, 60(1-2), 61-68.
D Chauhan et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell. 2012, 22(3), 345-358.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Inhibitor of deubiquitinase USP7 and USP47
Chemical name
1-(5-(2,3-dichlorophenylthio)-4-nitrothiophen-2-yl)ethanone
Parent CAS No.
[882257-11-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| GSK 461364 | Axon 1688
CAS [929095-18-1]
MF C27H28F3N5O2SMW 543.60
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Potent and selective Polo-like kinase (PLK) 1 inhibitor, more selective at PLK1 (Ki: 2.2 nM) over PLK2 and PLK3.
References
Certificates
Categories
Extra info
TR Rheault et al. Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophene carboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties. Bioorg. Med. Chem. Lett. 2010, 20(15), 4587-92.
KA Emmitte et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett. 2009, 19(6), 1694-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.11.21
PLK
PLK1 inhibitor
Chemical name
(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide
Parent CAS No.
[929095-18-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Aurora A inhibitor II | Axon 1630
CAS [1158838-43-7]
MF C31H29ClFN7O3MW 602.06
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 4.3 nM (Aurora A) and unusually high selectivity 860 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases
References
Certificates
Categories
Extra info
I Aliagas-Martin et al. A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J. Med. Chem. 2009, 52(10), 3300-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora A inhibitor
Chemical name
4-(2-(4-(2-(4-acetylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)-N-(2-chlorophenyl)benzamide
Parent CAS No.
[1158838-43-7]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| GSK 461364 analogue II | Axon 1626
CAS [929095-22-7]
MF C27H27F3N4O3SMW 544.59
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent Polo-like kinase (PLK) inhibitor, selective at PLK1 (IC50: 2 nM) over PLK3 (IC50: 270 nM)
References
Certificates
Categories
Extra info
TR Rheault et al. Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophene carboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties. Bioorg. Med. Chem. Lett. 2010, 20(15), 4587-92.
KA Emmitte et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett. 2009, 19(6), 1694-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
EC 2.7.11.21
PLK
PLK1 Inhibitor
Chemical name
(R)-5-(6-(1-methylpiperidin-4-yloxy)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide
Parent CAS No.
[929095-22-7]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| GSK 461364 analogue I | Axon 1625
CAS [929095-23-8]
MF C26H27ClN4O3SMW 511.04
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective Polo-like kinase (PLK) 1 inhibitor, more selective at PLK1 (IC50: 2 nM) over PLK3 (IC50: 630 nM)
References
Certificates
Categories
Extra info
TR Rheault et al. Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophene carboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties. Bioorg. Med. Chem. Lett. 2010, 20(15), 4587-92.
KA Emmitte et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett. 2009, 19(6), 1694-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.11.21
PLK
PLK1 Inhibitor
Chemical name
(R)-3-(1-(2-chlorophenyl)ethoxy)-5-(6-(1-methylpiperidin-4-yloxy)-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide
Parent CAS No.
[929095-23-8]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| Aurora A inhibitor I | Axon 1597
CAS [1158838-45-9]
MF C31H31ClFN7O2MW 588.07
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases. This ligand has much higher selectivity of Aurora A vs Aurora B than another recently described relatively selective Aurora A inhibitor MLN8054, which shows 43-fold selectivity for Aurora A over Aurora B in enzymatic assays
References
Certificates
Categories
Extra info
I Aliagas-Martin et al. A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J. Med. Chem. 2009, 52(10), 3300-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora A inhibitor
Chemical name
N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide
Parent CAS No.
[1158838-45-9]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| RO 3306 | Axon 1530
CAS [872573-93-8]
MF C18H13N3OS2MW 351.45
Purity:
99%
Soluble in DMSO
Description
Selective CDK 1 inhibitor (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively), which induces cell cycle arrest and actively enhances downstream p53 signaling to promote apoptosis in AML cell lines
References
Certificates
Categories
Extra info
LT Vassilev et al. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc Natl Acad Sci USA. 2006, 103(28), 10660–10665.
K Kojima et al. The CDK1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009, 100(6), 1128–1136.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK1 inhibitor
Chemical name
2-[[Thiophen-2-yl)methyl]amino]-5-[1-(quinolin-6-yl)meth-(Z)-ylidene]thiazol-4-one
Parent CAS No.
[872573-93-8]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| GW 843682X | Axon 1131
CAS [660868-91-7]
MF C22H18F3N3O4SMW 477.46
Purity:
99%
Soluble in DMSO
Description
Polo-like kinase (PLK) inhibitor; selective at PLK1 (IC50: 2 nM) and PLK3 (IC50: 9 nM)
References
Certificates
Categories
Extra info
EF Johnson et al. Pharmacological and Functional Comparison of the Polo-like Kinase Family: Insight into Inhibitor and Substrate Specificity. Biochemistry 2007, 46(33), 9558.
T Lansing et al. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol. Cancer Ther. 2007, 6, 450-459.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.11.21
PLK
PLK1 and PLK3 inhibitor
Chemical name
5-(5,6-Dimethoxy-benzoimidazol-1-yl-3-(2-trifluoromethyl-benzyloxy)-thiophene-2-carboxylic acid amide
Parent CAS No.
[660868-91-7]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| BI 6727 - Volasertib | Axon 1473
CAS [755038-65-4]
MF C34H50N8O3MW 618.81
Purity:
99%
Optical purity:
Optically pure
Moderately soluble in DMSO
Description
A highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines), which exhibited significant anti-proliferative in multiple cancer models, including a model of taxane-resistant colorectal cancer. A high volume of distribution, indicating good tissue penetration, and a long terminal half-life have emerged as distinct features of BI 6727, which may have a favorable effect on antitumor efficacy in vivo.
References
Certificates
Categories
Extra info
D Rudolph et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin. Cancer Res. 2009, 15(9), 3094-3102.
P Schöffski. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009, 14(6), 559-570.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
EC 2.7.11.21
PLK
PLK1 Inhibitor
Chemical name
N-((trans)-4-(4-(cyclopropylmethyl)piperazin-1-yl)cyclohexyl)-4-((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxybenzamide
Parent CAS No.
[755038-65-4]
Order
Size
Unit Price
Stock
2 mg
€90.00
In Stock | | axonmedchem |
| BI 2536 | Axon 1129
CAS [755038-02-9]
MF C28H39N7O3MW 521.65
Purity:
99%
Optical purity:
>99% ee
Soluble in DMSO
Description
Potent and selective polo-like kinase (PLK) 1 inhibitor.
KEYWORDS: BI 2536 | supplier | PLK1 inhibitor | BI2536 | BI-2536 | CAS [755038-02-9] | CHK2 | p53 | polo-like kinase | PLK-1 | malignancies | spindle assembly | mitotic arrest | apoptosis | anti-tumor | NSCLC | | axonmedchem |
| BAY 58-2667 hydrochloride - Cinaciguat hydrochloride | Axon 2172
CAS [646995-35-9]
MF C36H39NO5.HClMW 602.16
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent nitric oxide (NO)-independent soluble guanylyl cyclase (sGC) activator with haemodynamic effect similar to that of nitroglycerin (Ki value 6-8 nM in competition binding studies). Acts specifically on oxidized/haem-free sGC by binding to the enzyme's haem pocket and mimicking the nitric-oxide-bound haem group. BAY 58-2667 is in clinical development for the treatment of acute decompensated heart failure (ADHF).
KEYWORDS: BAY 58-2667 hydrochloride | supplier | sGC activator | Cinaciguat hydrochloride | BAY58-2667 | CAS [646995-35-9] | [329773-35-5] | GTP | sGC | soluble | guanylyl cyclase | NO | nitric oxide | heart failure | cardiac | ADHF | | axonmedchem |
| CK 1827452 - Omecamtiv Mecarbil | CK-452 | Axon 1835
CAS [873697-71-3]
MF C20H24FN5O3MW 401.43
Purity:
99%
Soluble in DMSO
Description
Selective cardiac specific myosin activator; clinically tested for its role in the treatment of left ventricular systolic heart failure.
KEYWORS: Omecamtiv Mecarbil | supplier | Myosin activator | CK 1827452 | CK-452 | CK1827452 | CAS [873697-71-3] | ATP | ATPase (cardiac specific myosin) | Activator | left ventricular systolic | heart failure | LVSHF | | axonmedchem |
| Digoxin - Digitalis | Axon 1649
CAS [20830-75-5]
MF C41H64O14MW 780.94
Purity:
98%
Soluble in DMSO
Description
Digoxin is a successful medication in the treatment of irregular heart rhythms, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication. Digoxin is also used as a standard control substance to test for p-glycoprotein inhibition. Recent studies show that digoxin acts as inhibitor of HIF-1α synthesis, reduces protein levels and thus slows tumor growth in mice
References
Certificates
Categories
Extra info
H Zhang et al. Digoxin and other cardiac glycosides inhibit HIF-1α synthesis and block tumor growth. Proc Natl Acad Sci USA 2008, 105, 19579-19586.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
ATPase (Na+K+)
EC 3.6.3.9
Na+/K+ ATPase pump inhibitor
Chemical name
4-((3S,5R,8R,9S,10S,12R,13S,14S,17S)-3-((2R,4S,5S,6R)-5-((2S,4S,5S,6R)-5-((2S,4S,5S,6R)-4,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yloxy)-4-hydroxy-6-methyltetrahydro-2H-pyran-2-yloxy)-4-hydroxy-6-methyltetrahydro-2H-pyran-2-yloxy)-12,14-dihydroxy-10,13-
Parent CAS No.
[20830-75-5]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Forskolin - Coleonol | Axon 2264
CAS [66575-29-9]
MF C22H34O7MW 410.50
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Activator of adenylate cyclase (IC50 value of 41 nM). A naturally occurring labdane diterpene that has been used extensively to increase cAMP and to elicit cAMP-dependent physiological responses. Elevation of cAMP levels by Forskolin induced neuronal differentiation of mesenchymal stem cells via activation of extracellular signal-regulated kinase/MAPK.
Anti-hypertensive and vasodilatory agent.
References
Certificates
Categories
Extra info
A. Laurenza et al. Forskolin: a specific stimulator of adenylyl cyclase or a diterpene with multiple sites of action? Trends Pharmacol Sci. 1989, 10, 442-447.
S.S. Kim et al. cAMP induces neuronal differentiation of mesenchymal stem cells via activation of extracellular signal-regulated kinase/MAPK. Neuroreport. 2005, 16, 1357-1361.
K. Seamon et al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J. Med. Chem., 1983, 26, 436–439.
J.D. Robbins et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J. Med. Chem. 1996, 39, 2745-2752.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Stem Cell
MAPK
Adenylate cyclase
EC 4.6.1.1
Stem Cell Differentiator
Activator of adenylate cyclase. Naturally occurring labdane diterpene
Chemical name
(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromen-5-yl acetate
Parent CAS No.
[66575-29-9]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| MYK-461 - Mavacamten | SAR439152 | Axon 2683
CAS [1642288-47-8]
MF C15H19N3O2MW 273.33
Purity:
100%
Optical purity:
Optically pure
Soluble in 0.1 N NaOH(aq) and DMSO
Description
MYK-461 is an inhibitor of sarcomere contraction by decreasing the ATPase activity of the cardiac myosin heavy chain (IC50 value 0.3 μM in mouse cardiac myofibrils). Inhibitors of sarcomere contraction may be a valuable therapeutic approach for hypertrophic cardiomyopathy (HCM). Acute reduction in contractility with MYK-461 is sufficient to relieve left ventricular outflow tract (LVOT) obstruction in feline HCM.
KEYWORDS: MYK-461 | supplier | Myosin inhibitor | MYK461 | MYK 461 | CAS [1642288-47-8] | ATP | ATPase (cardiac specific myosin) | Inhibitor | Enzymes | Sarcomere | HCM | LVOT | Hypertrophic Cardiomyopathy | Left Ventricular Outflow Tract | Myosin | | axonmedchem |
| Blebbistatin, (±)- | Axon 2718
CAS [674289-55-5]
MF C18H16N2O2MW 292.33
Purity:
99%
Soluble in DMSO
Description
Blebbistatin is a potent and specific inhibitor of the motor functions of class II myosins (IC50 values of 6.47, 3.58, 2.30 and 1.57 μM for inhibiting actin-activated ATPase activities of SmM, NM2a, NM2b and NM2c, respectively). Blebbistatin inhibited contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly. Moreover, Blebbistatin inhibited both the ATPase and gliding motility activities of human platelet nonmuscle myosin II without inhibiting myosin light chain kinase.
KEYWORDS: (±)-Blebbistatin | Myosin II inhibitor | Blebbistatin | CAS [674289-55-5] | ATP | ATPase (myosin) | Inhibitor | Enzymes | | axonmedchem |
| LRE1 - RU-0204277 | Axon 2664
CAS [1252362-53-0]
MF C12H13ClN4SMW 280.78
Purity:
98%
Soluble in DMSO
Description
LRE1 is an allosteric soluble adenylyl cyclase (sAC)-specific inhibitor (IC50 value ≤ 10μM). Inhibition occurs by occupying the binding site of the physiological activator HCO3-, preventing sAC-dependent processes in cellular and physiological systems. LRE1 also inhibited cAMP accumulation in 4-4 cells (IC50 value 11 μM). Overall, this sAC inhibitor combines high potency and selectivity with stability, solubility and lack of cytotoxicity.
KEYWORDS: LRE1 | Allosteric sAC inhibitor | supplier | RU-0204277 | LRE 1 | LRE-1 | RU 0204277 | RU0204277 | CAS [1252362-53-0] | ATP | Adenylate cyclase | Inhibitor | Enzymes | | axonmedchem |
| TAK 438 | Axon 1971
CAS [881681-01-2]
MF C17H16FN3O2S.C4H4O4MW 461.46
Purity:
98%
Soluble in DMSO
Description
Potassium-competitive acid blocker (P-CAB); reversibly inhibits gastric H+, K+-ATPase; TAK-438 exerts a longer and more potent antisecretory effect than lansoprazole as a result of its high accumulation and slow clearance from the gastric glands
References
Certificates
Categories
Extra info
J Matsukawa et al. A comparative study on the modes of action of TAK-438, a novel potassium-competitive acid blocker, and lansoprazole in primary cultured rabbit gastric glands. Biochem. Pharmacol. 2011, 81(9), 1145-1151.
JM Shin et al. Characterization of a novel potassium-competitive acid blocker of the gastric H,K-ATPase, 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine (...). J. Pharmacol. Exp. Ther. 2011, 339(2), 412-420.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
ATPase (H+K+)
EC 3.6.3.10
Potassium-competitive acid blocker (P-CAB)
Chemical name
1-(5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-N-methylmethanamine fumarate
Parent CAS No.
[881681-00-1]
Order
Size
Unit Price
Stock
5 mg
€145.00
In Stock | | axonmedchem |
| Digoxigenin bisdigitoxoside | Axon 1695
CAS [5297-05-2]
MF C35H54O11MW 650.80
Purity:
98%
Soluble in DMSO
Description
A metabolite of Digoxin (Axon 1649). Digoxin is a heart medication. Digoxin is also used as a standard control substance to test for p-glycoprotein inhibition. Recent studies show that digoxin acts as inhibitor of HIF-1α synthesis, reduces protein levels and thus slows tumor growth in mice.
KEYWORDS: Digoxigenin bis-digitoxiside | supplier | HIF-1 inhibitor | Digoxigenin bisdigitoxiside | CAS [5297-05-2] | ATP | ATPase (Na+K+) | Inhibitor | Enzymes | | axonmedchem |
| Fingolimod - FTY 720 | Axon 1485
CAS [162359-56-0]
MF C19H34ClNO2MW 343.93
Purity:
98%
Soluble in DMSO
Description
A sphingosine-1-phosphate receptor 1 modulator; immunosuppressant. FTY720 also activates the p21-activated kinase-1 (PAK1). Therefore, it could be a candidate therapeutic drug for the treatment of heart failure and arrhythmias.
References
Certificates
Categories
Extra info
EV Berdyshev et al. FTY720 inhibits ceramide synthases and up-regulates dihydrosphingosine 1-phosphate formation in human lung endothelial cells. J. Biol. Chem. 2009, 284(9), 5467–77.
KK Dev et al. Brain sphingosine-1-phosphate receptors: implication for FTY720 in the treatment of multiple sclerosis. Pharmacol. Ther. 2008, 117, 77-93.
K Chiba et al. Role of sphingosine 1-phosphate receptor type 1 in lymphocyte egress from secondary lymphoid tissues and thymus. Cell Mol. Immunol. 2006, 3, 11-19.
U Kunzendorf et al. FTY720—the first compound of a new promising class of immunosuppressive drugs. Nephrol. Dial. Transplant. 2004, 19, 1677-1681.
E.E. Egom et al. FTY720 prevents ischemia/reperfusion injury-associated arrhythmias in an ex vivo rat heart model via activation of Pak1/Akt signaling. J. Mol. Cell. Cardiol. 2010, 48, 406-414.
W. Liu et al. A novel immunomodulator, FTY-720 reverses existing cardiac hypertrophy and fibrosis from pressure overload by targeting NFAT (nuclear factor of activated T-cells) signaling and periostin. Circ Heart Fail. 2013 Jul;6(4):833-44.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cardiovascular
Immunology
Miscellaneous
Immunomodulator
S1PR1
A13
PAK
S1PR1 agonist; Immunosuppressant
Chemical name
2-Amino-2-[2-(4-octyl-phenyl)-ethyl]-propane-1,3-diol hydrochloride
Parent CAS No.
[162359-55-9]
Order
Size
Unit Price
Stock
10 mg
€60.00
In Stock | | axonmedchem |
| Olprinone hydrochloride - Loprinone hydrochloride | Axon 1168
CAS [119615-63-3]
MF C14H10N4O.HClMW 286.72
Purity:
99%
Soluble in water and DMSO
Description
Selective PDE III (PDE3) inhibitor; cardiotonic agent; with positive inotropic and vasodilating effects; as a therapeutic agent for acute heart failure.
KEYWORDS: Olprinone hydrochloride | supplier | PDE3 inhibitor | Loprinone hydrochloride | CAS [119615-63-3] | [106730-54-5] | cAMP | PDE | Inhibitor | Enzymes | | axonmedchem |
| NSC 59984 | Axon 2564
CAS [803647-40-7]
MF C12H15N3O4MW 265.27
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Activator of p53 that restores wild-type p53 signaling via p73 activation, specifically in mutant p53-expressing colorectal cancer cells, inducing cell death in colorectal cancer cells with minimal genotoxicity and without evident toxicity toward normal cells. Remarkebly, NSC 59984 induces degradation of several p53 mutants through MDM2-mediated ubiquitination.
KEYWORDS: NSC 59984 | supplier | p53 activator | NSC59984 | NSC-59984 | CAS [803647-40-7] | DNA-RNA | p53 | Activator | Transcription Factor | MDM2 | p73 | HDM | colorectal | cancer | ubiquitination | apoptosis | | axonmedchem |
| SCH 529074 | Axon 2244
CAS [922150-11-6]
MF C31H36Cl2N6MW 563.56
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Small molecule activator of mutant p53 which binds p53 DNA binding domain (DBD; Kd value 1-2 μM). SCH 529074 restores growth-suppressive function to mutant p53 (R273H and the structural mutant R249S) by acting as a chaperone and interrupts HDM2-mediated ubiquitination of wild type p53.
References
Certificates
Categories
Extra info
M. Demma et al. SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination (...). J. Biol. Chem. 2010, 285, 10198-10212.
F. Essmann et al. Translational approaches targeting the p53 pathway for anti-cancer therapy. Br. J. Pharmacol. 2012, 165, 328-344.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53
Transcription Factors
DNA-damage Response
Ubiquitin
TF class 4.3.1
Small molecule activator of mutant p53.
Chemical name
N1-(2-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine
Parent CAS No.
[922150-11-6]
Order
Size
Unit Price
Stock
5 mg
€100.00
In Stock | | axonmedchem |
| NSC 319726 | Axon 2016
CAS [71555-25-4]
MF C11H14N4SMW 234.32
Purity:
99%
Soluble in DMSO
Description
Reactivator of the p53 mutant p53R175; NSC319726 selectively kills cancer cells with a p53R175 mutations; it restores the transcriptional functions of p53R175
References
Certificates
Categories
Extra info
X Yu et al. Allele-Specific p53 Mutant Reactivation. Cancer Cell. 2012, 21(5), 614–625.
C Harrison. Anticancer drugs: Reactivating p53. Nature Reviews Drug Discovery 2012, 11, 517.
Mutant p53 Alleles Can Be Restored to the Wild-Type Conformation. Cancer Discovery 2012, 2(7), 581.
VV Prabhu et al. Therapeutic targeting of the p53 pathway in cancer stem cells. 2012, 16(12), 1161-1174.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53
Transcription Factors
DNA-damage Response
Ubiquitin
TF class 4.3.1
Reactivator of the p53 mutant p53R175
Chemical name
N'-(1-(pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide
Parent CAS No.
[71555-25-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Pifithrin-α hydrobromide - PFT-α | Axon 1871
CAS [63208-82-2]
MF C16H18N2OS.HBrMW 367.30
Purity:
99%
Soluble in DMSO
Description
Pifithrin-α is an inhibitor of p53 protein; reversibly blocks p53-dependent transcriptional activation and apoptosis; protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53
References
Certificates
Categories
Extra info
PG Komarov et al. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999, 285(5434), 1733-7.
PJM Murphy et al. Pifithrin-α Inhibits p53 Signaling after Interaction of the Tumor Suppressor Protein with hsp90 and Its Nuclear Translocation. J. Biol. Chem. 2004, 279, 30195-30201.
D Sohn et al. Pifithrin-α protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell Death and Differentiation. 2009, 16, 869–878.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
p53
Transcription Factors
DNA-damage Response
Ubiquitin
TF class 4.3.1
Stem Cell Differentiator
Inhibitor of p53 protein
Chemical name
2-(2-imino-4,5,6,7-tetrahydrobenzo[d]thiazol-3(2H)-yl)-1-p-tolylethanone hydrobromide
Parent CAS No.
[206983-57-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| JNJ 26854165 - Serdemetan | Axon 1538
CAS [881202-45-5]
MF C21H20N4MW 328.41
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Oral HDM2 inhibitor (or antagonist), which showed potent activity against multiple myeloma (MM) cells in vitro and ex vivo; potential agent to restore p53 function and to potentially impact other HDM2 dependent pathways.
Note: Its directly water soluble form, JNJ 26854165 dihydrochloride (Axon 1586), is also available.
KEYWORDS: JNJ26854165 | Supplier | HDM2 inhibitor | Serdemetan | JNJ26854165 | CAS [881202-45-5] | [881202-79-5] | p53 | HDM-MDM| Inhibitor | antagonist | multiple myeloma | MM | pathways | | axonmedchem |
| SP 141 | Axon 2437
CAS [1253491-42-7]
MF C15H11N3OMW 249.27
Purity:
99%
Soluble in DMSO
Description
Specific MDM2 inhibitor (Ki value 28 nM in a FP-based MDM2 binding assay) with potent therapeutic effects in breast cancer models, regardless of p53 status. SP141 directly binds to MDM2, inhibits MDM2 expression and induces its autoubiquitination and proteasomal degradation.
References
Certificates
Categories
Extra info
W. Wang et al. The pyrido[b]indole MDM2 inhibitor SP-141 exerts potent therapeutic effects in breast cancer models. Nat Commun. 2014 Oct 1;5:5086.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
DNA-damage Response
Ubiquitin
EC 6.3.2.19
HDM-MDM
Specific MDM2 inhibitor with therapeutic effects in breast cancer models
Chemical name
6-methoxy-1-(naphthalen-1-yl)-9H-pyrido[3,4-b]indole
Parent CAS No.
[1253491-42-7]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| SMURF1 inhibitor A01 - A01 | Axon 2426
CAS [1007647-73-5]
MF C22H20ClF3N4O3SMW 512.93
Purity:
99%
Soluble in DMSO
Description
SMAD ubiquitination regulatory factor-1 (SMURF1) E3 ubiquitin-protein ligase inhibitor (Kd value 3.7 nM), that strongly inhibits Smad1/5 ubiquitination under rhBMP-2 stimulation. A01 enhances BMP signaling responsiveness in C2C12 cells, and potentiates BMP-2 induced osteoblastic activity.
References
Certificates
Categories
Extra info
Y. Cao et al. Selective small molecule compounds increase BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. Sci Rep. 2014 May 14;4:4965.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Wnt-β-Catenin
MAPK
Ubiquitin
EC 6.3.2.19
Ubiquitin Ligase (E3; SMURF)
Inhibitor of E3 ubiquitin-protein ligase SMURF1
Chemical name
(4-(4-chloro-3-(trifluoromethyl)phenylsulfonyl)piperazin-1-yl)(4-(5-methyl-1H-pyrazol-1-yl)phenyl)methanone
Parent CAS No.
[1007647-73-5]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| SJ 172550 | Axon 2164
CAS [431979-47-4]
MF C22H21ClN2O5MW 428.87
Purity:
99%
Soluble in DMSO
Description
First small molecule inhibitor of MDMX with 10-fold selectivity over closely related MDM2 (EC50 2.3 μM vs 26.0 μM) which effectively kills MDMX-amplified retinoblastoma cells. SJ 172550 reversibly binds the p53-binding pocket of MDM, disrupts the MDMX-p53 interaction, and thereby frees p53 to induce apoptosis. The effect of SJ 172550 is additive when combined with an MDM2 inhibitor Nutlin 3a (Axon 1880). It may be useful for treating tumors that express wild-type p53
References
Certificates
Categories
Extra info
D Reed et al. Identification and characterization of the first small molecule inhibitor of MDMX. J. Biol. Chem. 2010, 285, 10786-10796.
JC Badciong et al. MdmX is a RING finger ubiquitin ligase capable of synergistically enhancing Mdm2 ubiquitination. J. Biol. Chem. 2002, 277, 49668-49675.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
EC 6.3.2.19
HDM-MDM
Small molecule inhibitor of MDMX
Chemical name
(E/Z)-methyl 2-(2-chloro-6-ethoxy-4-((3-methyl-5-oxo-1-phenyl-1H-pyrazol-4(5H)-ylidene)methyl)phenoxy)acetate
Parent CAS No.
[431979-47-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MLN 4924 - Pevonedistat | Axon 2038
CAS [905579-51-3]
MF C21H25N5O4SMW 443.52
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
First-in-class inhibitor of NEDD8 Activating Enzyme (NAE) with potent antitumor activity in animal models; cell permeable; MLN4924 inactivates Cullin-RING E3 ubiquitin Ligases (CRLs) by blocking cullin neddylation
References
Certificates
Categories
Extra info
TA Soucy et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 2009, 458, 732-736.
TA Soucy et al. Targeting NEDD8-Activated Cullin-RING Ligases for the Treatment of Cancer. Clin. Cancer Res. 2009, 15, 3912.
Y Zhao et al. Targeting Cullin-RING ligases by MLN4924 induces autophagy via modulating the HIF1-REDD1-TSC1-mTORC1-DEPTOR axis. Cell Death and Disease 2012, 3, e386.
JL Toth et al. A Gatekeeper Residue for NEDD8-Activating Enzyme Inhibition by MLN4924. Cell Reports, 2012, 1(4), 309-316.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Ubiquitin
EC 6.2.1
Ubiquitin Ligase (E1)
Inhibitor of NEDD8 Activating Enzyme (NAE)
Chemical name
((1S,2S,4R)-4-(4-((S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate
Parent CAS No.
[905579-51-3]
Order
Size
Unit Price
Stock
1 mg
€75.00
In Stock | | axonmedchem |
| RITA - NSC 652287 | Axon 2009
CAS [213261-59-7]
MF C14H12O3S2MW 292.37
Purity:
98%
Soluble in DMSO
Description
Small molecule p53 activator; MDM2 inhibitor
References
Certificates
Categories
Extra info
MN Saha et al. RITA Inhibits Multiple Myeloma Cell Growth through Induction of p53-Mediated Caspase-Dependent Apoptosis and Synergistically Enhances Nutlin-Induced Cytotoxic Responses. Mol. Cancer Ther. 2010, 9, 3041.
N Issaeva et al. Small molecule RITA binds to p53, blocks p53−HDM-2 interaction and activates p53 function in tumors. Nature Med. 2004, 10, 1321-1328.
MN Saha et al. Targeting p53 via JNK pathway: a novel role of RITA for apoptotic signaling in multiple myeloma. PLoS One. 2012, 7(1), e30215.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
DNA-damage Response
Ubiquitin
EC 6.3.2.19
HDM-MDM
Activates p53 through inhibition of MDM2
Chemical name
(5,5'-(furan-2,5-diyl)bis(thiophene-5,2-diyl))dimethanol
Parent CAS No.
[213261-59-7]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| PRT 4165 - NSC 600157 | Axon 1953
CAS [31083-55-3]
MF C15H9NO2MW 235.24
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
E3 Ubiquitin ligase Bmi1/Ring1A inhibitor
References
Certificates
Categories
Extra info
I Alchanati et al. The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex - a potentially new drug target. PLoS One. 2009, 4(12), e8104.
L Bedford et al. Ubiquitin-like protein conjugation and the ubiquitin–proteasome system as drug targets. Nat. Rev. Drug Discov. 2011, 10, 29-46.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Ubiquitin Ligase (E3; SCF family)
Ubiquitin
EC 6.3.2.19
E3 Ubiquitin ligase Bmi1/Ring1A inhibitor
Chemical name
2-(pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione
Parent CAS No.
[31083-55-3]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| SMER 3 | Axon 1904
CAS [67200-34-4]
MF C11H4N4O2MW 224.18
Purity:
99%
Soluble in DMSO
Description
Specific inhibitor of an SCF family E3 Ubiquitin ligase, directly targeting the Met30 subunit of the SCF family E3 ubiquitin ligase complex; Small molecule enhancer of rapamycin (SMER)
References
Certificates
Categories
Extra info
M Aghajan et al. Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase Nat. Biotechnol. 2010, 28, 738-742.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Ubiquitin Ligase (E3; SCF family)
Ubiquitin
EC 6.3.2.19
Inhibitor of an SCF family E3 Ubiquitin ligase
Chemical name
9H-indeno[1,2-e][1,2,5]oxadiazolo[3,4-b]pyrazin-9-one
Parent CAS No.
[67200-34-4]
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10 mg
€90.00
In Stock | | axonmedchem |
| Nutlin-3b - Nutlin-3, (+)- | Axon 1881
CAS [675576-97-3]
MF C30H30Cl2N4O4MW 581.49
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Nutlin-3b is a 150-fold less potent (+)-enantiomer of Nutlin-3 (Axon 1585) as p53 MDM2 antagonist or inhibitor, in comparison with more potent opposite (-)-enantiomer Nutlin-3a (Axon 1880); useful as a negative control for non-Mdm2 related cellular activities.
KEYWORDS: Nutlin-3b | MDM2 inhibitor | Nutlin-3, (+)- | Nutlin3b | Nutlin3 | Nutlin 3b | Nutlin 3 | CAS [675576-97-3] | p53 | HDM-MDM | Inhibitor | Enzymes | | axonmedchem |
| Nutlin-3a - Nutlin-3, (-)- | Axon 1880
CAS [675576-98-4]
MF C30H30Cl2N4O4MW 581.49
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Nutlin-3a is an antagonist or inhibitor of MDM2 (human homolog of murine double minute 2), which disrupts its interaction with p53, leading to the stabilization and activation of p53.
*Note: Nutlin-3a (Axon 1880) is the 150-fold more potent (-)-enantiomer of Nutlin-3 (Axon 1585), in comparision with the opposite (+)-enantiomer Nutlin-3b (Axon 1881). Presently, much attention has been given to Nutlin-3a and its absolute stereo-assignment is now known.
References
Certificates
Categories
Extra info
V Manfé et al. MDM2 Inhibitor Nutlin-3a Induces Apoptosis and Senescence in Cutaneous T-Cell Lymphoma: Role of p53. J. Invest. Dermatol. 2012, 132, 1487-1496.
E Drakos et al. Activation of the p53 pathway by the MDM2 inhibitor nutlin-3a overcomes BCL2 overexpression in a preclinical model of diffuse large B-cell lymphoma associated with t(14;18)(q32;q21). Leukemia 2011, 25, 856–867.
F Zhang et al. MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport. Biochem. Pharmacol. 2011, 82(1), 24-34.
H Hasegawa et al. Activation of p53 by Nutlin-3a, an antagonist of MDM2, induces apoptosis and cellular senescence in adult T-cell leukemia cells. Leukemia 2009, 23, 2090–2101.
TA Davis and JN Johnston. Catalytic, enantioselective synthesis of stilbene cis-diamines: A concise preparation of (-)-Nutlin-3, a potent p53/MDM2 inhibitor. Chem. Sci. 2011, 2, 1076-1079.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
Ubiquitin
EC 6.3.2.19
HDM-MDM
Inhibitor of MDM2
Chemical name
4-((4S,5R)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one
Parent CAS No.
[675576-98-4]
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Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| HLI 373 | Axon 1643
CAS [N.A.]
MF C18H23N5O2.2HClMW 414.33
Purity:
98%
Soluble in water and DMSO
Description
A water soluble and potent Hdm2 inhibitor that inhibits the ubiquitin ligase activity of Hdm2, stabilizes p53 and activates p53-dependent transcription, and induces cell death; HLI 373 is effective in inducing apoptosis of several tumor cells lines that are sensitive to DNA-damaging agents
References
Certificates
Categories
Extra info
J Kitagaki et al. Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2. Mol. Cancer Ther. 2008, 7(8), 2445–2454.
Y Yang et al. Targeting the ubiquitin-proteasome system for cancer therapy. Cancer Sci. 2009, 100(1), 24-28.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
Ubiquitin
EC 6.3.2.19
HDM-MDM
HDM2 inhibitor
Chemical name
5-(3-(dimethylamino)propylamino)-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione hydrochloride
Parent CAS No.
[502137-98-6]
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Size
Unit Price
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5 mg
€95.00
In Stock | | axonmedchem |
| Nutlin-3 | Axon 1585
CAS [548472-68-0]
MF C30H30Cl2N4O4MW 581.49
Purity:
99%
Soluble in DMSO and Ethanol
Description
MDM2 antagonist, which binds MDM2 in the p53-binding pocket and activates the p53 pathway in cancer cells, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts in nude mice.
Note: Its two enantiomers, more active (-)-enantiomer Nutlin-3a (Axon 1880) and less active (+)-enantiomer Nutlin-3b (Axon 1881), are also available.
References
Certificates
Categories
Extra info
LT Vassilev et al. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2. Science 2004, 303, 844-848.
S Shangary and S Wang. Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction to Reactivate p53 Function: A Novel Approach for Cancer Therapy. Ann. Rev. Pharmacol. Toxicol. 2008, 49: 223–241.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Transcription Factors
p53-Tumor Suppression
Ubiquitin
EC 6.3.2.19
HDM-MDM
MDM2 inhibitor (p53 specific)
Chemical name
4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one
Parent CAS No.
[548472-68-0]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| JTP 1048196 | Axon 2947
CAS [55377-56-5]
MF C17H14O4MW 282.29
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| Bexarotene - SR 11247 | Targretin | Axon 1700
CAS [153559-49-0]
MF C24H28O2MW 348.48
Purity:
99%
Soluble in DMSO
Description
Selective agonist for retinoid X receptors (RXR); An oral antineoplastic agent indicated for cutaneous T cell lymphoma (CTCL)
References
Certificates
Categories
Extra info
R Gniadecki et al. The optimal use of bexarotene in cutaneous T-cell lymphoma. Br. J. Dermatol. 2007, 157(3), 433–440.
KH Dragnev et al. A proof-of-principle clinical trial of bexarotene in patients with non-small cell lung cancer. Clin Cancer Res. 2007, 13(6), 1794-800.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Retinoic Acid (RXR)
NR2B
Retinoid X Receptor antagonist
Chemical name
4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid
Parent CAS No.
[153559-49-0]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |