| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Temozolomide - TMZ | NSC 362856 | SCH 52365 | CCRG 81045 | Axon 2326
CAS [85622-93-1]
MF C6H6N6O2MW 194.15
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Chemotherapeutic apoptosis inducer. An orally active alkylating agent prodrug, delivering a methyl group to purine bases of DNA (O6-guanine; N7-guanine and N3-adenine). Temozolomide has demonstrated efficacy in the treatment of a variety of solid tumors, primary malignant brain tumors and metastatic melanoma (IC50 value 5 μM for cytotoxicity against mouse TLX5 lymphoma cells).The primary cytotoxic lesion, O6-methylguanine (O6-MeG) can be removed by methylguanine methyltransferase (MGMT; direct repair) in tumours expressing this protein, or tolerated in mismatch repair-deficient (MMR-) tumours.
References
Certificates
Categories
Extra info
J. Zhang et al. Temozolomide: mechanisms of action, repair and resistance. Curr. Mol. Pharmacol. 2012, 5, 102-114.
H.S. Friedman et al. Temozolomide and treatment of malignant glioma. Clin. Cancer Res. 2000, 6, 2585-2597.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
DNA-damage Response
DNA
DNA methylating agent; apoptosis inducer
Chemical name
3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
Parent CAS No.
[85622-93-1]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| UCB-L 060 - Etiracetam, R-(+)- | Axon 1111
CAS [103765-01-1]
MF C8H14N2O2MW 170.21
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO
Description
Acetylcholine agonist; less active enantiomer of Etiracetam (Axon 1109), in comparison with (S)-(-)-enantiomer, Levetiracetam (Axon 1110)
References
Certificates
Categories
Extra info
Hovinga CA: Levetiracetam: a novel antiepileptic drug. Pharmacotherapy 2001, 21(11), 1375-1388.
Certificate of Analysis
Material Safety Data Sheet
CNS
SV2A
Unclassified
Least active enantiomer of Axon 1109
Chemical name
(R)-2-(2-Oxo-pyrrolidin-1-yl)-butyramide
Parent CAS No.
[103765-01-1]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| LY 573636 - Tasisulam | Axon 1963
CAS [519055-62-0]
MF C11H6BrCl2NO3S2MW 415.11
Purity:
98%
Soluble in DMSO
Description
Anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo; LY573636 is selectively toxic towards tumor cells over their normal counterparts
References
Certificates
Categories
Extra info
T Haritunians et al. Novel acyl sulfonamide LY573636-sodium: effect on hematopoietic malignant cells. Oncol Rep. 2008, 20(5), 1237-1242.
JM Kirkwood et al. A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma. Cancer 2011, 117(20), 4732–4739.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
Anti-tumor agent; causes growth arrest and apoptosis
Chemical name
N-(5-bromothiophen-2-ylsulfonyl)-2,4-dichlorobenzamide
Parent CAS No.
[519055-62-0]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Dimethylcelecoxib, 2,5- - DMC | Axon 2496
CAS [457639-26-8]
MF C18H16F3N3O2SMW 395.40
Purity:
100%
Soluble in DMSO
Description
Celecoxib analog that lacks COX-2 inhibitory activity but exhibits anti-tumor properties; DMC reduced growth and initiated apoptotic cell death in several MM cell lines. Mechanistically, DMC down-regulates critical components of the cell-cycle machinery (cyclins A and B); blocks the activity of important mitogenic and survival pathways (MEK, NF-κB, STAT3, survivin); and leads to increased caspase activity. Moreover, DMC quite potently mimics the ability of celecoxib to stimulate the endoplasmic reticulum stress response (ESR) and subsequent cell death .
References
Certificates
Categories
Extra info
A. Kardosh et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood. 2005 Dec 15;106(13):4330-8.
A. Kardosh et al. Dimethyl-celecoxib (DMC), a derivative of celecoxib that lacks cyclooxygenase-2-inhibitory function, potently mimics the anti-tumor effects of celecoxib on Burkitt's lymphoma in vitro and in vivo. Cancer Biol Ther. 2005 May;4(5):571-82.
P. Pyrko et al. Calcium-activated endoplasmic reticulum stress as a major component of tumor cell death induced by 2,5-dimethyl-celecoxib, a non-coxib analogue of celecoxib. Mol Cancer Ther. 2007 Apr;6(4):1262-75.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
NF-κB
MAPK
JAK-STAT
Unclassified
Celecoxib analog with anti-tumor properties, lacking COX-2 inhibitory activity
Chemical name
4-(5-(2,5-dimethylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide
Parent CAS No.
[457639-26-8]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| VU 0029767 | Axon 1988
CAS [326001-01-8]
MF C21H21N3O3MW 363.41
Purity:
98%
Soluble in DMSO
Description
Positive allosteric modulator of M1. VU 0029767 potentiates the agonistic effect of ACh for M1 (Ki value shifted by VU0029767 (3, 10 and 30 M) and shifted the ACh competition curve by 1.7 0.8-, 4.9 2.0-, and 8.8 1.9-fold, respectively, compared to control (DMSO; Ki value 8.7 µM). VU0029767 potentiates ACh-mediated intracellular calcium mobilization, but not phospholipase D activation.
References
Certificates
Categories
Extra info
J.E. Marlo et al. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol Pharmacol. 2009 Mar;75(3):577-88.
P.J. Conn et al. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci. 2009 Mar;30(3):148-55.
Certificate of Analysis
Material Safety Data Sheet
CNS
CHRM1
A18
PAM of mAChR M1 that potentiates the agonistic effect of Ach
Chemical name
(E)-2-(4-ethoxyphenylamino)-N'-((2-hydroxynaphthalen-1-yl)methylene)acetohydrazide
Parent CAS No.
[326001-01-8]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| BMS 605541 | Axon 2837
CAS [639858-32-5]
MF C19H17F2N5OSMW 401.43
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| NVP-ACC789 - ACC789 | ZK 202650 | Axon 2865
CAS [300842-64-2]
MF C21H17BrN4MW 405.29
Purity:
99%
Soluble in DMSO
Description
NVP-ACC789 is a VEGFR2 inhibitor (IC50 value of 0.02 µM) moderately active against VEGFR1 and VEGFR3, but has little activity against PDGFR-β tyrosine kinases. Blocks angiogenesis induced by VEGF in vivo and in vitro.
KEYWORDS: NVP-ACC789 | supplier | VEGFR2 inhibitor | ACC789 | ZK 202650 | ACC-789 | ACC 789 | ZK-202650 | ZK202650 | CAS [300842-64-2] | VEGF | VEGFR | Inhibitor | Receptors | Angiogenesis | | axonmedchem |
| Stem Cell 5i inhibitor Set | Axon 5007
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of five small molecule pathway inhibitors, BMP inhibitor LDN 193189 hydrochloride (Axon 1509), TGF-beta inhibitor SB 431542 (Axon 1661) and GSK3 inhibitor CHIR 99021 (Axon 1386), FGFR inhibitor SU 5402 (Axon 1667) and Gamma secretase inhibitor DAPT (Axon 1484) (termed as stem cell 5i or LSB3i or LSB+3i inhibitor set), for neural differentiation of human pluripotent stem cells (hPSCs). Stem Cell 5i (or LSB3i) inhibitor cocktail protocol, actually a combination of LSB inhibitor set (Axon 5004) and neuronal 3i (CSD) inhibitor set (Axon 5006), was used for rapid and efficient differentiateing hPSCs into nociceptors.
Read more: Additional Product Information
Show all Axon Ligand™ Sets
References
Certificates
Categories
Extra info
S.M. Chambers et al. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature Biotechnol. 2012, 30, 715-720.
List of publications using LDN 193189 hydrochloride (Axon 1509) purchased from Axon Medchem
List of publications using CHIR 99021 (Axon 1386) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Angiogenesis
Apoptosis
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
VEGFR
GSK-3
mTOR
γ Secretase
Wnt-β-Catenin
TGF-β
PI3K-Akt-mTOR
Stem Cells
Stem Cell Differentiator
BMP-ALK
FGFR
TGF-βR
Set of five inhibitors for neural differentiation of human pluripotent stem cells.
Chemical name
N.A.
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
Each 2 mg
€220.00
In Stock | | axonmedchem |
| J147 | Axon 2859
CAS [1146963-51-0]
MF C18H17F3N2O2MW 350.33
Purity:
100%
Soluble in DMSO
Description
J147 is a potent and orally active neurotrophic drug that facilitates memory in normal rodents. Moreover, J147 prevents the loss of synaptic proteins and cognitive decline in a transgenic AD mouse model. Neuroprotectant.
KEYWORDS: J147 | supplier | Neurotrophic drug | J 147 | J-147 | CAS [1146963-51-0] | Metabolism | Neuroprotectants | Alzheimer | Cognitive Enhancement | Neurodegenerative | | axonmedchem |
| Stem Cell CSD inhibitor Set | Axon 5006
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of three small molecule inhibitors, GSK-3 inhibitor CHIR 99021 (Axon 1386), FGFR inhibitor SU 5402 (Axon 1667) and gamma secretase inhibitor DAPT (Axon 1484) (termed as CSD or neuronal 3i). CHIR 99021 is the key factor for inducing neuronal differentiation, whereas SU 5402 and DAPT further enhance efficiency.
Combination of stem cell CSD (neuronal 3i) inhibitor set with LSB inhibitor set (Axon 5004) forms stem cell 5i inhibitor set (Axon 5007, aka LSB3i or LSB+3i), which was used for rapid and efficient differentiation of human pluripotent stem cells (hPSCs) into nociceptors.
Read more: Additional Product Information
Show all Axon Ligand™ Sets
References
Certificates
Categories
Extra info
S.M. Chambers et al. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature Biotechnol. 2012, 30, 715-720.
List of publications using CHIR 99021 (Axon 1386) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Angiogenesis
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
VEGFR
GSK-3
γ Secretase
Wnt-β-Catenin
PI3K-Akt-mTOR
Stem Cells
Stem Cell Differentiator
FGFR
Set of CHIR 99021, SU5402, and DAPT, inhibitors of GSK-3, FGFR, and γ-secretase, resp.
Chemical name
N.A.
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
Each 2 mg
€155.00
In Stock | | axonmedchem |
| XL 388 | Axon 2951
CAS [1251156-08-7]
MF C23H22FN3O4SMW 455.50
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Recently added | | axonmedchem |
| SUVN-502 | Axon 2715
CAS [1791396-46-7]
MF C23H32BrN3O9S3MW 670.61
Purity:
99%
Soluble in water and DMSO
Description
SUVN-502 is a potent, selective and orally active serotonin 6 (5-HT6) receptor antagonist (Ki value of 2.04 nM) with selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins. Moreover, it has high selectivity over 5-HT2A receptor. SUVN-502 is brain penetrant and a clinical candidate for potential treatment of cognitive disorders.
KEYWORDS: SUVN-502 | supplier | 5-HT6 antagonist | SUVN502 | SUVN 502 | CAS [1791396-46-7] | [701205-60-9] | Serotonin | 5-HT6 | Antagonist | Receptors | Alzheimer | | axonmedchem |
| S-Propargyl-Cysteine - SPRC | ZYZ-802 | Axon 2666
CAS [3262-64-4]
MF C6H9NO2SMW 159.21
Purity:
98%
Optical purity:
Optically pure
Soluble in water
Description
S-Propargyl-cysteine (SPRC), a substrate of cystathionine γ-lyase (CSE), is a water-soluble modulator of endogenous hydrogen disulfide (H2S). SPRC is a potential agent for the treatment of Alzheimer’s disease (TNF signalling, the NF-κB pathway and the ERK1/2 pathway), anemia of inflammation (IL-6/JAK2/STAT3 pathway), ischemic heart disease (H2S/VEGFR2/STAT3 pathway) and myocardial infarction.
KEYWORDS: S-Propargyl-Cysteine | supplier | H2S donor | SPRC | ZYZ-802 | S-Propargylcysteine | ZYZ802 | ZYZ 802 | CAS [3262-64-4] | L-cysteine | CSE | Activator | Enzymes | | axonmedchem |
| eCF309 | Axon 2630
CAS [2001571-40-8]
MF C18H21N7O3MW 383.40
Purity:
98%
Moderately soluble in DMSO
Description
Potent inhibitor of mTOR signalling (IC50 value 10 - 15 nM in vitro and in vivo) with very high selectivity over other kinases, including PI3Ks. The selectivity profile of eCF309 is as good as or even better than that of any other selective mTOR inhibitor reported to date, making it a highly valuable probe for chemical biology and biomedicine.
Note: | | axonmedchem |
| Lu AE58054 hydrochloride - Idalopirdine HCl | Axon 2144
CAS [467458-02-2]
MF C20H19F5N2O.HClMW 434.83
Purity:
100%
Soluble in water and DMSO
Description
5-HT6 receptor antagonist (Ki value 0.83 nM for h5-HT6) demonstrating >50-fold selectivity for more than 70 targets examined, with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Idalopirdine (Lu AE58054) potentiates the effects of Donepezil (Axon 1438) on two pharmacodynamic biomarkers associated with cognition, i.e. neuronal oscillations and extracellular ACh levels in the hippocampus.
Note | | axonmedchem |
| 5-HT6 antagonist 29 | Axon 1575
CAS [497963-70-9]
MF C19H20ClN3O2S.HClMW 426.36
Purity:
99%
Soluble in DMSO
Description
Selective brain penetrant 5-HT6 receptor antagonist (pKi value 8.6). Close regio-isomer of SB 699929 with brain–blood ratio of 2.6:1 and ED50 value of 5 mg/kg (po), and thus twice as potent as SB 271046 (Axon 1099).
References
Certificates
Categories
Extra info
M. Ahmed et al. Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists. Bioorg. Med. Chem. Lett. 2005, 15, 4867-4871.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
Selective brain penetrant 5-HT6 receptor antagonist
Chemical name
3-(4-chlorophenylsulfonyl)-1-methyl-7-(piperazin-1-yl)-1H-indole hydrochloride
Parent CAS No.
[478082-77-8]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| SGS 518 | Axon 1927
CAS [445441-26-9]
MF C21H22F2N2O3SMW 420.47
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT6 antagonist, being developed as a treatment for Cognitive Impairment Associated with Schizophrenia (CIAS)
References
Certificates
Categories
Extra info
C Wilson, AV Terry. Enhancing cognition in neurologic disorders: Potential usefulness of 5-HT6 antagonists. Drugs Fut. 2009, 34(12), 969.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
Selective 5-HT6 antagonist
Chemical name
1-methyl-3-(1-methylpiperidin-4-yl)-1H-indol-5-yl 2,6-difluorobenzenesulfonate
Parent CAS No.
[445441-26-9]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| MS 245 oxalate | Axon 1849
CAS [275363-58-1]
MF C19H22N2O3S.C2H2O4MW 448.49
Purity:
99%
Soluble in DMSO
Description
Selective and high affinity 5-HT6 antagonist (Ki = 2.1 nM)
References
Certificates
Categories
Extra info
Y Tsai et al. N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. Bioorg Med Chem Lett. 2000, 10(20), 2295-2299.
R Young et al. Effect of the 5-HT(6) serotonin antagonist MS-245 on the actions of (-)nicotine. Pharmacol. Biochem. Behav. 2006, 85(1), 170-1777.
M Dukat et al. Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. J. Med. Chem. 2008, 51, 603.
RVS Nirogi et al. Novel and potent 5-piperazinyl methyl-N1-aryl sulfonyl indole derivatives as 5-HT6 receptor ligands. ACS Med. Chem. Lett. 2010, 1, 340.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
5-HT6 antagonist
Chemical name
2-(5-methoxy-1-(phenylsulfonyl)-1H-indol-3-yl)-N,N-dimethylethanamine oxalate
Parent CAS No.
[263384-65-2]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| WAY 208466 dihydrochloride | Axon 1710
CAS [1207064-61-6]
MF C17H18FN3O2S.2HClMW 420.33
Purity:
99%
Soluble in water
Description
Potent and highly selective serotonin 5-HT6 receptor agonist (EC50: 7.3 nM); increases GABA levels in the cerebral cortex; produces antidepressant and anxiolytic effects in rodents; useful in the treatment of obsessive-compulsive disorder (OCD)
References
Certificates
Categories
Extra info
LE Schechter et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology 2008, 33, 1323–1335.
GV Carr et al. Antidepressant and anxiolytic effects of selective 5-HT(6) receptor agonists in rats. Psychopharmacology 2010, 213(2–3), 499–507.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
Potent and selective 5-HT6 receptor agonist
Chemical name
2-(3-(3-fluorophenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-1-yl)-N,N-dimethylethanamine dihydrochloride
Parent CAS No.
[633304-27-5]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| RO 04-6790 hydrochloride | Axon 1330
CAS [1197333-95-1]
MF C12H16N6O2S.2HClMW 381.28
Purity:
98%
Soluble in 0.1N HCl(aq)
Description
Potent and selective serotonin 5-HT6 receptor antagonist
References
Certificates
Categories
Extra info
AJ Sleight et al. Characterization of Ro 04-6790 and Ro 63-0563: Potent and selective antagonists at human and rat 5-HT6 receptors. Br. J. Pharmacol. 1998, 124, 556-562.
JC Bentley et al. Investigation of stretching behavior induced by the selective 5-HT6 receptor antagonist Ro 04-6790 in rats. Br. J. Pharmacol. 1999, 126, 1537-1542.
Lindner, M.D. et al. An assessment of the effects of serotonin 6 (5-HT6) Receptor antagonists in rodent models of learning. J. Pharmacol. Exp. Ther. 2003, 307(2), 682-691.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
5-HT6 antagonist
Chemical name
4-Amino-N-(2,6-bis-methylamino-pyrimidin-4-yl)-benzenesulfonamide hydrocholoride
Parent CAS No.
[202466-68-0]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Olanzapine - LY 170053 | Axon 1298
CAS [132539-06-1]
MF C17H20N4SMW 312.43
Purity:
99%
Soluble in DMSO
Description
Atypical antipsychotic; Higher affinity for 5-HT2 receptors than D2 receptors. D1/D2/D4/5-HT2C antagonist. Also nanomolar affinity for 5-HT6/5-HT7 receptors. Weak activity on dopamine sites, appears to bind to M3 and M4 receptor sites. Anticholinergic and anxiolytic properties
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT6
5-HT7
5-HT2C
5-HT2
D4
CHRM3
D1
CHRM4
CHRM1
A17
Atypical antipsychotic
Chemical name
2-Methyl-10-(4-methyl-piperazin-1-yl)-4H-3-thia-4,9-diaza-benzo[f]azulene
Parent CAS No.
[132539-06-1]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SB 271046 hydrochloride | Axon 1099
CAS [209481-24-3]
MF C20H22ClN3O3S2.HClMW 488.45
Purity:
99%
Soluble in DMSO
Description
Putative 5-HT6 antagonist
References
Certificates
Categories
Extra info
SM Bromidge et al. 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J. Med. Chem. 1999, 42(2), 202-5.
C Routledge et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br. J. Pharmacol. 2000, 130(7), 1606-1612.
AG Foley et al. The 5-HT(6) receptor antagonist SB-271046 reverses scopolamine-disrupted consolidation of a passive avoidance task and ameliorates spatial task deficits in aged rats. Neuropsychopharmacol. 2004, 29(1), 93-100.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
A17
5-HT6 antagonist
Chemical name
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid (4-methoxy-3-piperazin-1-yl-phenyl)-amide hydrochloride
Parent CAS No.
[209481-20-9]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| VA012 | Axon 2889
CAS [885898-58-8]
MF C21H19N3MW 313.40
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| MHY 1485 | Axon 2425
CAS [326914-06-1]
MF C17H21N7O4MW 387.39
Purity:
99%
Soluble in DMSO
Description
mTOR activator with an inhibitory effect on autophagy. MHY1485 markedly increased the LC3II/LC3I ratio dose-dependently and time-dependently by inhibition of the fusion between autophagosomes and lysosomes, and without increasing the autophagic flux. At 2 µM, MHY1485 did not show any cell death during longer treatment, supporting that MHY1485 had less toxicity than other well-known inhibitors of autophagy. MHY1485 was also tested and found moderately active as antimalarial agent (MIC value of ca. 26 µM against P. Falciparum).
References
Certificates
Categories
Extra info
Y.J. Choi et al. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion. PLoS One. 2012;7(8):e43418.
A. Agarwal et al. Syntheses of 2,4,6-trisubstituted triazines as antimalarial agents. Bioorg Med Chem Lett. 2005 Feb 1;15(3):531-3.
H. Ojha et al. Quantitative structure activity relationship study of 2,4,6-trisubstituted-s-triazine derivatives as antimalarial inhibitors of Plasmodium falciparum dihydrofolate reductase. Chem Biol Drug Des. 2011 Jan;77(1):57-62.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Immunology
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Antiprotozoal agents
Autophagy
mTOR activator with an inhibitory effect on autophagy
Chemical name
4,6-dimorpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine
Parent CAS No.
[326914-06-1]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| Bifeprunox mesylate - DU 127090 | Axon 1508
CAS [350992-13-1]
MF C24H23N3O2.CH4O3SMW 481.56
Purity:
98%
Soluble in DMSO
Description
Dopamine D2 and 5-HT1A partial agonist in development as a potential treatment for schizophrenia and other psychotic indications; Pharmacoloy profile makes it an atypical antipsychotic and a new approach for the treatment of schizophrenia.
KEYWORDS: Bifeprunox mesylate | Supplier | D2/5-HT1A agonist | DU 127090 | DU127090 | DU-127090 | CAS [350992-13-1] | [350992-10-8] | Serotonin | Dopamine | D2 | 5-HT1A | schizophrenia | psychotic indications | atypical | antipsychotic | extrapyramidal symptoms | | axonmedchem |
| WAY 100635 maleate | Axon 2424
CAS [1092679-51-0]
MF C25H34N4O2.C4H4O4MW 538.64
Purity:
98%
Soluble in water and DMSO
Description
Prototypical 5-HT1A receptor antagonist with D4 agonist activity (Ki values 2.2 nM, 6260 nM, 24 nM, >10,000 nM, 20 nM, 322 nM, and 16 nM for 5-HT1A, 5-HT2A, 5-HT2B, 5-HT7, α1A, α1B, and D4, respectively).
The HCl salt of WAY 100635 is available as well (Axon 1086)
References
Certificates
Categories
Extra info
B.R. Chemel et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51.
EA Forster et al. A pharmacological profile of the selective silent 5-HT1A receptor antagonist WAY-100635. Eur. J. Pharmacol. 1995, 281, 81-88.
F. Mangin et al. Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4550-4.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
5-HT1A
D4
Adrenoceptor α1
A19
5-HT1A antagonist with D4 agonistic properties
Chemical name
Cyclohexanecarboxylic acid {2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-pyridin-2-yl-amide maleate
Parent CAS No.
[162760-96-5]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| IITZ-01 | Axon 2933
CAS [1807988-47-1]
MF C26H23FN8OMW 482.51
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| MSL-7 | Axon 2932
CAS [2172949-70-9]
MF C16H12ClNO4SMW 349.79
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| A 381393 | Axon 2944
CAS [726174-00-1]
MF C20H24N4MW 320.43
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Recently added | | axonmedchem |
| QX77 | Axon 2902
CAS [1798331-92-6]
MF C16H13ClN2O2MW 300.74
Purity:
98%
Soluble in DMSO
Description
Chaperone-mediated autophagy (CMA) activator. QX77 operates through the release of the endogenous inhibition of the retinoic receptor-α signaling pathway over the regulation of multiple mechanisms that modulate CMA.
KEYWORDS: QX77 | supplier | CMA activator | QX 77 | QX-77 | CAS [1798331-92-6] | Retinoic Acid | Retinoic Acid (RAR) | Antagonist | Receptors | Cystinosis | LAMP2A | Cystinosin | | axonmedchem |
| Sonepiprazole hydrochloride - PNU 101387 | Axon 2115
CAS [170857-36-0]
MF C21H27N3O3S.HClMW 437.98
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Selective dopamine D4 antagonist; Displayed high affinity (Ki = 10 nM) and selectivity for the D4 receptor expressed in clonal cell lines, lacking measurable affinity for other dopamine receptors, and noradrenalin, serotonin and histamine receptor families (Ki > 2000 nM)
References
Certificates
Categories
Extra info
PA Broderick et al. Clozapine, haloperidol, and the D4 antagonist PNU-101387G: in vivo effects on mesocortical, mesolimbic, and nigrostriatal dopamine and serotonin release. J. Neural. Transm. 1998, 105(6-7), 749-767.
KM Merchant et al. Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J. Pharmacol. Exp. Ther. 1996, 279(3), 1392-1403.
Certificate of Analysis
Material Safety Data Sheet
CNS
D4
A17
Pfizer Licensed Products
Selective dopamine D4 antagonist
Chemical name
(S)-4-(4-(2-(isochroman-1-yl)ethyl)piperazin-1-yl)benzenesulfonamide hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[170858-33-0]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| STF 62247 | Axon 2894
CAS [315702-99-9]
MF C15H13N3SMW 267.35
Purity:
99%
Soluble in DMSO
Description
STF 62247 selectively targets VHL-deficient renal cell carcinoma (RCC) cells (IC50 value of 0.625 µM in RCC4). STF 62247-stimulated toxicity occurs in a HIF-independent manner through autophagy. Moreover, STF 62247 induced apoptotic and autophagic cell death in leukemic cells.
Keywords: STF 62247 | supplier | Inducer of apoptosis and autophagy | STF-62247 | STF62247 | CAS [315702-99-9] | Smad | Ubiquitin Ligase (E3; VHL) | Inducer | Enzymes | VHL | RCC | Leukemia | ATL | HTLV-1 | | axonmedchem |
| LY 2955303 dihydrochloride | Axon 2637
CAS [N.A.]
MF C36H42N4O3.2HClMW 651.67
Purity:
99%
Soluble in DMSO
Description
Potent and selective retinoic acid receptor gamma (RARγ) antagonist (Ki values >1700 nM, >2980 nM, and 1.1 nM for RARα, RARβ, and RARγ, respectively) for the treatment of osteoarthritis joint pain.
KEYWORDS: LY 2955303 dihydrochloride | supplier | RARγ antagonist | LY2955303 diHCl | LY-2955303 dihydrochloride | CAS [N.A.] | [1433497-19-8] | Retinoic Acid | Retinoic Acid (RAR) | Nuclear receptors | NR1B | osteoarthritis | pain | Antagonist | Receptors | | axonmedchem |
| JTP 0819958 - HOIPIN-1 | Axon 2939
CAS [N.A.]
MF C17H13NaO4MW 304.27
Purity:
99%
Soluble in water and DMSO
Recently added | | axonmedchem |
| UNC 9994 hydrochloride | Axon 2562
CAS [N.A.]
MF C21H22Cl2N2OS.HClMW 457.84
Purity:
99%
Soluble in DMSO
Description
Unique, β-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in β-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in β-arrestin-2 knockout mice.
KEYWORDS: UNC 9994 hydrochloride | supplier | D2 agonist | Axon Medchem | Axon 2562 | UNC9994 | CAS [1354030-51-5] | Dopamine | D2 | Agonist | GPCR | D2R | β-arrestin | beta-arrestin | antipsychotic | | axonmedchem |
| NRX 194204 - IRX4204 | NRX 4204 | VTP 194204 | AGN 194204 | AGN 4204 | Axon 2408
CAS [220619-73-8]
MF C24H32O2MW 352.51
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Highly potent and specific RXR agonist (Kd values 0.4 nM, 3.6 nM, and 3.8 nM for RXRα, RXRβ, and RXRγ, respectively) devoid of any RAR activity (Kd values >30 µM for RARα, RARβ, and RARγ). NRX 194204 blocked the ability of lipopolysaccharide and TNFα to induce the release of nitric oxide and IL6 and the degradation of IKBα in RAW264.7 macrophage-like cells. NRX194204 prevents carcinogenesis in both the lung and mammary gland, and enhances the ability of ligands for PPARs or cytotoxic drugs, including cisplatin and 5-flurouracil, to inhibit proliferation and induce apoptosis in breast and pancreatic cancer cell lines.
KEYWORDS: NRX 194204 | RXR agonist | NRX 4204 | VTP 194204 | AGN 194204 | AGN 4204 | NRX4204;NRX-4204; IRX 4204; IRX-4204 | NRX194204; NRX-194204 | VTP194204; VTP-194204 | AGN194204; AGN-194204 | AGN4204; AGN-4204 | CAS [220619-73-8] | Retinoic Acid | Retinoic Acid (RXR) | devoid | RAR | carcinogenesis | Agonist | Receptors | | axonmedchem |
| SAR405838 - MI-77301 | Axon 2741
CAS [1303607-60-4]
MF C29H34Cl2FN3O3MW 562.50
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
SAR405838 is an inhibitor of the MDM2-p53 interaction with high specificity over other proteins (Ki value of 0.88 nM). SAR405838 effectively activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell-cycle arrest and/or apoptosis. At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer, and HCT-116 colon cancer.
KEYWORDS: SAR405838 | supplier | MDM2 inhibitor | MI-77301 | SAR 405838 | SAR-405838 | MI 77301 | MI77301 | CAS [1303607-60-4] | p53 | HDM-MDM | Inhibitor | Enzymes | Apoptosis | | axonmedchem |
| NS 30678 hydrochloride | Axon 1742
CAS [1193707-19-5]
MF C12H16ClNO4S.HClMW 342.24
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Dopamine D2 receptor ligand with surmountable/competitive-like D2 antagonist properties (Ki and IC50 values of value 9.7 nM and 7 nM, repectively in HEK-hD2L-Gαqi5 cells), equipotent to Haloperidol and Risperidone (Axon 1454). NS30678 shows rapid recovery and dopamine responsiveness within 5 min after administration.
References
Certificates
Categories
Extra info
T. Dyhring et al. The dopaminergic stabilizers pridopidine (ACR16) and (-)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties. Eur J Pharmacol. 2010 Feb 25;628(1-3):19-26.
K. Sahlholm et al. Typical and atypical antipsychotics do not differ markedly in their reversibility of antagonism of the dopamine D2 receptor. Int J Neuropsychopharmacol. 2014 Jan;17(1):149-55.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
A17
D2 ligand with surmountable/competitive-like D2 antagonist properties
Chemical name
(S)-N-((5-chloro-7-(methylsulfonyl)-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)ethanamine hydrochloride
Parent CAS No.
[1193707-15-1]
Order
Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| AMG 232 | Axon 2639
CAS [1352066-68-2]
MF C28H35Cl2NO5SMW 568.55
Purity:
100%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent, selective, and orally bioavailable MDM2-p53 inhibitor (IC50 value 9.1 nM, Kd 0.045 nM), demonstrating remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model. Moreover, AMG 232 activates p53 pathway activity in vivo, and potentiates the activity of p53-inducing cytotoxic agents.
KEYWORDS: AMG 232 | supplier | MDM2 inhibitor | AMG232 | AMG-232 | CAS [1352066-68-2] | Axon Medchem | Axon 2639 | p53 | HDM-MDM | orally bioavailable | MDM2-p53 interaction | antitumor activity | SJSA-1 | osteosarcoma | xenograft model | p21 | | axonmedchem |
| N106 | Axon 2565
CAS [862974-25-2]
MF C17H14N4O3SMW 354.38
Purity:
99%
Soluble in DMSO
Description
First-in-class small-molecule activator targeting E1 ligase mediated SERCA2a SUMOylation. N106 treatment increases contractile properties of cultured rat cardiomyocytes and significantly improves ventricular function in mice with heart failure.
KEYWORDS: N106 | supplier | E1 ligase activator | N-106 | CAS [862974-25-2] | Ubiquitin | Ubiquitin Ligase (E1) | Activator | small ubiquitin-like modifier type 1 | SUMO-1 | SERCA2a | SUMOylation | heart failure | cardiomyocyte | cardiac | sarcoplasmic reticulum | calcium | ATPase | | axonmedchem |
| JNJ 26854165 dihydrochloride - Serdemetan dihydrochloride | Axon 1586
CAS [881202-16-0]
MF C21H20N4.2HClMW 401.33
Purity:
99%
Soluble in water 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: JNJ 26854165 dihydrochloride is a directly water-soluble form of JNJ 26854165 (Axon 1538)
KEYWORDS: JNJ26854165 dihydrochloride | Supplier | HDM2 inhibitor | Serdemetan dihydrochloride | JNJ26854165 | CAS [881202-16-0] | [881202-45-5] | p53 | HDM-MDM | Inhibitor | antagonist | multiple myeloma | MM | pathways | | axonmedchem |
| CC-885 | Axon 2645
CAS [1010100-07-8]
MF C22H21ClN4O4MW 440.88
Purity:
99%
Soluble in DMSO
Description
Cereblon (CRBN) modulator with potent anti-tumour activity which is mediated through the cereblon-dependent ubiquitination and degradation of the translation termination factor GSPT1. CC-885 exhibits potent anti-proliferative activity in patient-derived acute myeloid leukaemia (AML) tumour cell lines.
KEYWORDS: CC-885 | supplier | Cereblon (CRBN) modulator | CC885 | CAS [1010100-07-8] | Ubitquitin | signaling | E3 ligase | GSPT1 | CRL4 | DDB1 | CUL4 | AML | myeloid leukaemia | | axonmedchem |
| CDN1163 | Axon 2684
CAS [892711-75-0]
MF C20H20N2O2MW 320.39
Purity:
100%
Soluble in DMSO
Description
CDN1163 is an allosteric activator of sarco/endoplasmic reticulum Ca2+-ATPase 2b (SERCA2b) and markedly lowered fasting blood glucose, improved glucose tolerance, and ameliorated hepatosteatosis in a genetic model of insulin resistance and type 2 diabetes (ob/ob mice). CDN1163 treatment significantly reduced the hepatic expression of genes involved in gluconeogenesis and lipogenesis, attenuated ER stress response and ER stress-induced apoptosis, and improved mitochondrial biogenesis. Moreover, CDN1163 increased ER calcium content, rescued neurons from ER stress-induced cell death in vitro, and showed significant efficacy in the rat 6-hydroxydopamine (6-OHDA) model of Parkinson's disease.
KEYWORDS: CDN1163 | supplier | SERCA activator | CDN 1163 | CDN-1163 | CAS [892711-75-0] | ATP | ATPase (Ca2+) | Activator | Enzymes | SERCA | 6-OHDA | Obesitas | Diabetes | Metabolic Disorder | Metabolic Dysfunction | ER Stress | Parkinson's Disease | | axonmedchem |
| Tenovin 1 | Axon 2008
CAS [380315-80-0]
MF C20H23N3O2SMW 369.48
Purity:
99%
Soluble in DMSO
Description
p53 activator that has the potential to decrease tumor growth; Tenovin 1 acts through inhibition of the protein-deacetylating activities of SIRT1 and SIRT2, two important members of the sirtuin family
References
Certificates
Categories
Extra info
S Lain et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008, 13(5), 454-463.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
DNA-damage Response
EC 3.5.1.98
SIRT
Activates p53 through inhibition of SIRT 1 and 2
Chemical name
N-(4-acetamidophenylcarbamothioyl)-4-tert-butylbenzamide
Parent CAS No.
[380315-80-0]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| LDN 57444 | Axon 2449
CAS [668467-91-2]
MF C17H11Cl3N2O3MW 397.64
Purity:
99%
Soluble in DMSO
Description
Reversible, competitive inhibitor of UCH-L1 (Ki value 0.40 µM; IC50 values 0.88 µM and 25 µM for UCH-L1 and UCH-L3 inhibition, respectively), that promotes proliferation of H1299 NSCLC cells and SH-SY5Y neuroblastoma cells. A usefull tool to study the role of UCH-L1 in Parkinson’s disease, cancer, and neuropathic pain.
References
Certificates
Categories
Extra info
Y. Liu et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem Biol. 2003 Sep;10(9):837-46.
UCH-L1 inhibition involved in CREB dephosphorylation in hippocampal slices. M Xie et al. J Mol Neurosci. 2014 May;53(1):59-68.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Pain & Inflammation
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Reversible, competitive inhibitor of UCH-L1 deubiquitinase
Chemical name
3-(acetoxyimino)-5-chloro-1-(2,5-dichlorobenzyl)indolin-2-one
Parent CAS No.
[668467-91-2]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| OSS-128167 | Axon 2843
CAS [887686-02-4]
MF C19H14N2O6MW 366.32
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
OSS-128167 is a selective SIRT6 inhibitor (IC50 value of 89 µM).
KEYWORDS: OSS-128167 | supplier | SIRT 6 inhibitor | OSS128167 | OSS 128167 | CAS [887686-02-4] | Histone | SIRT | Inhibitor | Enzymes | Sirtuin | Diabetes | | axonmedchem |
| TCID | Axon 2333
CAS [30675-13-9]
MF C9H2Cl4O2MW 283.92
Purity:
99%
Soluble in DMSO
Description
Potent, cell permeant inhibitor of UCHL3 (IC50 value 0.6 µM) with 125-fold selectivity over UCHL1. Specific inhibition of UCHL3 with TCID diminished GlyT2 ubiquitination in brainstem and spinal cord primary neurons and may be beneficial in several human disorders, including neuromotor deficiencies (startle disease, myoclonus), pain and epilepsy.
References
Certificates
Categories
Extra info
Y. Liu et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem. Biol. 2003, 10, 837-846.
J. de Juan-Sanz et al. Constitutive endocytosis and turnover of the neuronal glycine transporter GlyT2 is dependent on ubiquitination of a C-terminal lysine cluster. PLoS One. 2013, 8, e58863.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Ubiquitin
EC 3.4.19.12
Deubiquitinase
Potent inhibitor of UCHL3 with >100-fold selectivity over UCHL1
Chemical name
4,5,6,7-tetrachloro-1H-indene-1,3(2H)-dione
Parent CAS No.
[30675-13-9]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| ML364 | Axon 2678
CAS [1991986-30-1]
MF C24H18F3N3O3S2MW 517.54
Purity:
99%
Soluble in DMSO
Description
ML364, a small molecule inhibitor of the deubiquitinase USP2 (IC50 value of 1.1 μM), induced an increase in cellular cyclin D1 degradation and caused cell cycle arrest. Consistent with the role of cyclin D1 in DNA damage response, ML364 also caused a decrease in homologous recombination-mediated DNA repair. These effects by a small molecule inhibitor support a key role for USP2 as a regulator of cell cycle, DNA repair, and tumor cell growth.
KEYWORDS: ML364 | supplier | USP2 inhibitor | ML 364 | ML-364 | CAS [1991986-30-1] | Non Selective (Ubiquitin peptides) | Deubiquitinase | Inhibitor | Enzymes | | axonmedchem |
| ONX 0914 - PR 957 | Axon 2199
CAS [960374-59-8]
MF C31H40N4O7MW 580.67
Purity:
98%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective inhibitor of LMP7, the chymotrypsin-like subunit of the immunoproteasome. ONX 0914 blocks the production of cytokines IL-23, TNF-α, and IL-6 in a NF-κB independent manner, and attenuates progression of experimental arthritis in mouse models.ONX 0914 induces an anti-inflammatory response at doses less than one tenth of the maximum tolerated dose, in contrast to nonselective inhibitors, such as bortezomib (Axon 1810) and carfilzomib.
References
Certificates
Categories
Extra info
T. Muchamuel et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis. Nat. Med. 2009, 15, 781-788.
S.E. Verbrugge et al. Inactivating PSMB5 Mutations and P-Glycoprotein (Multidrug Resistance-Associated Protein/ATP-Binding Cassette B1) Mediate Resistance to Proteasome Inhibitors: Ex Vivo Efficacy of (...). J. Pharmacol. Exp. Ther. 2012, 341, 174-182.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Immunomodulator
Proteasome 26S
Ubiquitin
EC 3.4
Selective inhibitor of LMP7 subunit of the immunoproteasome.
Chemical name
(S)-3-(4-methoxyphenyl)-N-((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide
Parent CAS No.
[960374-59-8]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| Bortezomib - PS 341 | Axon 1810
CAS [179324-69-7]
MF C19H25BN4O4MW 384.24
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Highly selective and reversible inhibitor of the 26S proteasome; a chemotherapy agent used in the treatment of multiple myeloma; shown to have anti-tumor activity in B cell malignancies
References
Certificates
Categories
Extra info
P Bonvini et al. Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma. Leukemia 2007, 21(4), 838–842.
S Williams et al. Differential effects of the proteasome inhibitor bortezomib on apoptosis and angiogenesis in human prostate tumor xenografts. Mol. Cancer Ther. 2003, 2, 835-843.
Y Ling et al. Mechanisms of Proteasome Inhibitor PS-341-induced G2-M-Phase Arrest and Apoptosis in Human Non-Small Cell Lung Cancer Cell Lines. Clin. Cancer Res. 2003, 9, 1145-1154.
A Corso et al. Bortezomib plus dexamethasone can improve stem cell collection and overcome the need for additional chemotherapy before autologous transplant in patients with myeloma. Leukemia & Lymphoma 2010, 51(2), 236-242.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Proteasome 26S
Ubiquitin
EC 3.4
Inhibitor of 26S proteasome
Chemical name
(R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butan-2-ylboronic acid
Parent CAS No.
[179324-69-7]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |