| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| SB 706504 - PCG | Axon 2444
CAS [911110-38-8]
MF C24H19F3N8OMW 492.46
Purity:
98%
Soluble in DMSO
Description
Selective p38-MAPK inhibitor that targets a subset of inflammatory macrophage genes (IC50 value 2.5 nM for p38α, and no IC50 values below 5 μM, except for JNK1 (5 µM)). When used with dexamethasone, SB 706504 causes effective suppression of these genes without affecting transcription of a subset of LPS-regulated genes, including IL-1β, IL-18, and CCL5 (genes involved in the pathogenesis of COPD). Furthermore, SB 706504 reduces TNFα, GM-CSF, and IL-6 production from LPS-stimulated COPD macrophages, with less effect on IL-8 production.
KEYWORDS: SB 706504 | Supplier | p38 MAPK inhibitor | Axon Medchem | Axon 2444 | PCG | SB706504 | CAS [911110-38-8] | MAPK (p38) | Inhibitor | COPD | macrophage | inflammation | LPS | TNFα | cytokines | | axonmedchem |
| U 0126 - U 126 | Axon 2520
CAS [109511-58-2]
MF C18H16N6S2MW 380.49
Purity:
99%
Soluble in DMSO and Ethanol
Description
Non-competitive inhibitior of the dual specificity kinase MEK (IC50 values 0.07 μM and 0.06 μM for MEK1 and MEK2, respectively) that protects the brain against damage resulting from ischemic stroke in mice. U0126 is frequently used in combination with PD 98059 (Axon 1223), and both are found to accelerate differentiation of murine RAW264.7 cells into osteoclast-like cells.
KEYWORDS: U 0126 | Supplier | MEK1/2 inhibitor | U 126 | U0126 | U126 | CAS [109511-58-2] | [1173097-76-1] | MAPK | MEK | Inhibitor | Ischemia | stroke | differentiation | osteoclast-like cells | | axonmedchem |
| Enzastaurin - LY 317615 | Axon 1682
CAS [170364-57-5]
MF C32H29N5O2MW 515.60
Purity:
99%
Soluble in DMSO
Description
Selective protein kinase C β (PKC-β) inhibitor; Enzastaurin inhibits PKC-β, PKCα, PKCγ and PKCε with IC50 values of 6, 39, 83 and 110 nM, respectively
References
Certificates
Categories
Extra info
JR Graff et al. The Protein Kinase Cβ–Selective Inhibitor, Enzastaurin (LY317615.HCl), Suppresses Signaling through the AKT Pathway, Induces Apoptosis, and Suppresses Growth of Human Colon Cancer (...). Cancer Res. 2005, 65, 7462-7469.
MA Rizvi et al. Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. Mol. Cancer Ther. 2006, 5, 1783-1789.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
NF-κB
PI3K-Akt-mTOR
EC 2.7.11.13
PKC
PKC-β inhibitor
Chemical name
3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Parent CAS No.
[170364-57-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| BMS 582949 | Axon 2856
CAS [623152-17-0]
MF C22H26N6O2MW 406.48
Purity:
98%
Soluble in DMSO
Description
BMS 582949 is a highly selective p38α MAP kinase inhibitor (IC50 value of 13 nM).
KEYWORDS: BMS 582949 | supplier | p38 MAPK inhibitor | BMS582949 | BMS-582949 | CAS [623152-17-0] | MAP kinase | MAPK | MAPK (p38) | Inhibitor | Enzymes | p38α | | axonmedchem |
| PXS 4728A - PXS 4728 HCl | Axon 2583
CAS [1478364-68-9]
MF C15H21FN2O2.HClMW 316.80
Purity:
98%
Soluble in water and DMSO
Description
Potent and orally available inhibitor of VAP-1 (aka SSAO/AOC3; IC50 value 5 nM), inhibiting neutrophil rolling and tethering in the mouse cremaster model, and showing >500-fold selectivity for VAP-1/SSAO over all the related human amine oxidases. PXS 4728 diminishes lung inflammation in a variety of models indicating proof of concept for a novel therapeutic approach in respiratory diseases that are characterized by neutrophilic pattern of inflammation. PXS 4728 is in clinical trials for the treatment of cardiometabolic diseases like the liver-related disease Nonalcoholic Steatohepatitis (NASH).
KEYWORDS: PXS 4728A | supplier | VAP-1 inhibitor | PXS 4728 HCl | PXS4728 | CAS [1478364-68-9] | [1478364-40-7] | Mono-amines | VAP | Inhibitor | SSAO | AOC3 | neutrophil | adhesion molecules | VAP-1/SSAO | lung inflammation | COPD | airway | respiratory | steatohepatitis | NASH | liver disease | Semicarbazide Sensitive Amine Oxidase | | axonmedchem |
| LY 333531 hydrochloride - Ruboxistaurin | Axon 2362
CAS [169939-93-9]
MF C28H28N4O3.HClMW 505.01
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally active protein kinase C β (PKC-β) specific inhibitor; the more water soluble mesylate salt of LY 333531 (Axon 1401) is available as well.
KEYWORDS: LY 333531 HCl | supplier | PKC-β inhibitor | Ruboxistaurin | LY333531 | LY-333531 | CAS [169939-93-9] | [169939-94-0] | protein kinase | PKC-beta | orally active | ICAM-1 | MCP-1 | diabetes | glutathion | retinopathy | | axonmedchem |
| CID 2011756 | Axon 1976
CAS [638156-11-3]
MF C22H21ClN2O3MW 396.87
Purity:
99%
Soluble in DMSO
Description
ATP-competitive and cell-permeable protein kinase D (PKD) inhibitor
References
Certificates
Categories
Extra info
ER Sharlow et al. Discovery of Diverse Small Molecule Chemotypes with Cell-Based PKD1 Inhibitory Activity. PLoS ONE 2011, 6(10), e25134.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
EC 2.7.11.13
PKD
ATP-competitive and cell-permeable PKD inhibitor
Chemical name
5-(3-chlorophenyl)-N-(4-(morpholinomethyl)phenyl)furan-2-carboxamide
Parent CAS No.
[638156-11-3]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| CID 755673 | Axon 1627
CAS [521937-07-5]
MF C12H11NO3MW 217.22
Purity:
98%
Soluble in DMSO
Description
Selective protein kinase D (PKD) inhibitor
References
Certificates
Categories
Extra info
ER Sharlow et al. Potent and Selective Disruption of Protein Kinase D Functionality by a Benzoxoloazepinolone. J. Biol. Chem. 2008, 283, 33516-33526.
E Torres-Marquez et al. CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway. Biochem. Biophys. Res. Commun. 2010, 391(1), 63-68.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
EC 2.7.11.13
PKD
PKD inhibitor
Chemical name
7-hydroxy-2,3,4,5-tetrahydro-1H-benzofuro[2,3-c]azepin-1-one
Parent CAS No.
[521937-07-5]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Roflumilast - Daxas | BY 217 | BYK 20869 | B 9302-107 | Axon 2352
CAS [162401-32-3]
MF C17H14Cl2F2N2O3MW 403.21
Purity:
100%
Soluble in DMSO
Description
First specific PDE4 inhibitor (IC50 value 0.2 - 4.3 nM for inhibition of PDE4 subtypes) licensed for the treatment of COPD.
References
Certificates
Categories
Extra info
K.F. Rabe et al. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br. J. Pharmacol. 2011, 163, 53-67.
W. Timmer et al. The new phosphodiesterase 4 inhibitor roflumilast is efficacious in exercise-induced asthma and leads to suppression of LPS-stimulated TNF-alpha ex vivo. J. Clin. Pharmacol. 2002, 42, 297-303.
L.A. Sorbera et al. Roflumilast: antiallergy/antiasthmatic, treatment of COPD, phosphodiesterase 4 inhibitor. Drugs Fut. 2000, 25, 1261-1264.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.53
PDE
First specific PDE4 inhibitor licensed for treatment of COPD
Chemical name
3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
Parent CAS No.
[162401-32-3]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| GSK 2256294A - GSK 2256294 | Axon 2220
CAS [1142090-23-0]
MF C21H24F3N7OMW 447.46
Purity:
99%
Optical purity:
Optically pure (absolute stereochemistry)
Soluble in DMSO
Description
GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (IC50 value 27 pM), and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH. GSK2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in a cell line transfected with the human sEH enzyme.The selectivity of the compound has been demonstrated by testing against a large panel of enzymes, receptors and ion channels, including the phosphatase activity of EPHX2.
References
Certificates
Categories
Extra info
P.L. Podolin et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013, 104-105, 25-31.
L.A. Morgan et al. Soluble epoxide hydrolase inhibition does not prevent cardiac remodeling and dysfunction after aortic constriction in rats and mice. J. Cardiovasc. Pharmacol. 2013, 61, 291-301.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
Pain & Inflammation
sEH
NF-κB
EC 3.3.2.10
Potent, reversible, tight binding inhibitor of recombinant human sEH
Chemical name
(1R,3S)-N-(4-cyano-2-(trifluoromethyl)benzyl)-3-(4-methyl-6-(methylamino)-1,3,5-triazin-2-ylamino)cyclohexanecarboxamide
Parent CAS No.
[1142090-23-0]
Order
Size
Unit Price
Stock
2 mg
€125.00
In Stock | | axonmedchem |
| BPKDi | Axon 2798
CAS [1201673-28-0]
MF C21H28N6OMW 380.49
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
BPKDi is an inhibitor of protein kinase D (IC50 values of 1, 9, and 1 nM for PKD1, PKD2 and PKD3, respectively). BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes and concomitantly suppresses hypertrophy of these cells.
KEYWORDS: BPKDi | supplier | PKD inhibitor | CAS [1201673-28-0] | Non Selective (Phosphorylation Substrates) | PKD | Inhibitor | Enzymes | Cardiac Class IIa HDAC | | axonmedchem |
| PF 956980 | Axon 2217
CAS [1262832-74-5]
MF C18H26N6OMW 342.44
Purity:
98%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
JAK3 inhibitor and close analogue of CP 690550 (Tofacitinib; Axon 1338 and Axon 2072). Useful tool compound to study JAK3 inhibition in the treatment of various diseases, particularly asthma and COPD, and rheumatoid arthritis.
References
Certificates
Categories
Extra info
A.J. Steele et al. The JAK3-selective inhibitor PF-956980 reverses the resistance to cytotoxic agents induced by interleukin-4 treatment of chronic lymphocytic leukemia cells: potential for reversal of (...). Blood 2010, 116(22), 4569-4577.
P.S. Changelian et al. The specificity of JAK3 kinase inhibitors. Blood, 2008, 111(4), 2155-2157.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
JAK-STAT
EC 2.7.10.2
JAK
Pfizer Licensed Products
JAK3 inhibitor; analogue of Axon 1338 and 2072
Chemical name
((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)(pyrrolidin-1-yl)methanone
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1262832-74-5]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| PDE9A inhibitor C33(S) - (S)-C33 | Axon 2825
CAS [2066488-39-7]
MF C18H20ClN5OMW 357.84
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
(S)-C33 is a potent and selective PDE9A inhibitor with an IC50 value of 11 nM.
KEYWORDS: PDE9A inhibitor C33(S) | supplier | PDE9A inhibitor | (S)-C33 | CAS [2066488-39-7] | cGMP | PDE | Inhibitor | Enzymes | PDE9 | PDE9A | | axonmedchem |
| TAK 063 | Axon 2399
CAS [1238697-26-1]
MF C23H17FN6O2MW 428.42
Purity:
99%
Soluble in DMSO
Description
Highly potent, and orally active PDE10A inhibitor (IC50 value 0.30 nM) with excellent selectivity (>15000-fold selective over other PDEs). TAK-063 represents a promising drug for the treatment of schizophrenia with potential for superior safety and tolerability profiles.
KEYWORDS: TAK 063 | Supplier | PDE10A inhibitor | TAK063 | CAS [1238697-26-1] | cGMP | PDE | Inhibitor | phosphodiesterase | schizofrenia | antipsychotic | orally active | cAMP | cGMP | | axonmedchem |
| ARM1 hydrobromide | Axon 2307
CAS [1049743-03-4]
MF C16H14N2S.HBrMW 347.27
Purity:
99%
Soluble in DMSO
Description
Novel type of LTA4H inhibitor (IC50 value of ~0.5 μM in human neutrophils, and Ki value of 2.3 μM for purified LTA4H) that selectively blocks the conversion of LTA4 into proinflammatory mediator LTB4, although leaving the aminopeptidase activity intact for cleavage and inactivation of Pro-Gly-Pro.About LTA4H: Leukotriene A4 hydrolase/aminopeptidase (LTA4H) is a bifunctional zinc metalloenzyme that catalyzes biosynthesis of the proinflammatory mediator, LTB4, implicated in chronic inflammatory diseases. Recently, the chemotactic tripeptide Pro-Gly-Pro was identified as the enzyme’s endogenous peptidase substrate.
KEYWORDS: ARM1 hydrobromide | supplier | LTA4H inhibitor | ARM1 HBr | CAS [1049743-03-4] | [68729-05-5] | Eicosanoid epoxides | LTA4H | Inhibitor | neutrophils | LTA4 | proinflammatory mediator | LTB4 | aminopeptidasePro-Gly-Pro | inflammation | | axonmedchem |
| Cerdulatinib - PRT 062070 | Axon 2775
CAS [1198300-79-6]
MF C20H27N7O3SMW 445.54
Purity:
98%
Soluble in DMSO
Description
Cerdulatinib is an orally active kinase inhibitor that demonstrates activity against Syk and JAK with IC50 values of 32 nM, 12 nM, 6 nM and 8 nM for Syk, JAK1, JAK2 and JAK3, respectively. Cellular assays demonstrated specific inhibitory activity against signaling pathways that use Syk and JAK1/3. Limited inhibition of JAK2 was observed. Potent antitumor activity was observed in a subset of B-cell lymphoma cell lines.
KEYWORDS: Cerdulatinib | support | Syk/JAK inhibitor | PRT 062070 | PRT062070 | PRT-062070 | CAS [1198300-79-6] | CAS [1369761-01-2] | B-Cell Transformation | Spleen tyrosine kinase (Syk) | JAK | Inhibitor | Enzymes | B-cell lymphoma | | axonmedchem |
| Parogrelil - NT 702, free base | NM 702 | Axon 1482
CAS [139145-27-0]
MF C19H18BrClN4O2MW 449.73
Purity:
99%
Soluble in DMSO
Description
Selective and potent PDE III (PDE3) inhibitor; a new type of agent with both a bronchodilating and an anti-inflammatory effect
References
Certificates
Categories
Extra info
M Hori et al. NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase 3 inhibitor, suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. Eur. J. Pharmacol. 2009, 618(1-3), 63-69.
N Ishiwata. NT-702, a novel and potent phosphodiesterase inhibitor, improves reduced walking distance and lowered hindlimb plantar surface temperature in a rat experimental intermittent claudication model. Life Sci. 2007, 81(12), 970-978.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.17
PDE
PDE3 inhibitor
Chemical name
4-bromo-6-[3-(4-chlorophenyl)propoxy]-5-[(pyridin-3-ylmethyl)amino]-2,3-dihydropyridazin-3-one
Parent CAS No.
[139145-27-0]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| NVP-BSK805 - BSK 805 | Axon 2792
CAS [1092499-93-8 ]
MF C27H28F2N6OMW 490.55
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
NVP-BSK805 is a potent, selective and orally bioavailable JAK2 inhibitor (IC50 value of 7.3 nM) with very good solubility and cellular potency. Moreover, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.
Keywords: NVP-BSK805 | supplier | JAK2 inhibitor | BSK 805 | NVP BSK805 | NVPBSK805 | BSK805 | BSK-805 | CAS [1092499-93-8 ] | JAK-STAT Pathway | JAK | Inhibitor | Enzymes | Polycythemia | Erythropoiesis | | axonmedchem |
| Dimethylenastron - Eg5 inhibitor III | Axon 2439
CAS [863774-58-7]
MF C16H18N2O2SMW 302.39
Purity:
98%
Optical purity:
Racemate
Soluble in DMSO
Description
Specific potent and cell-permeable inhibitor of the mitotic motor Eg5 (a.k.a. kinesin-5 or KSP; IC50 value 200 nM). Dimethylenastron proved to be >100-times more potent than monastrol, both in vitro and with arresting mitosis of cultured cells. Capable of halting cell cycle progression in mitosis and of inducing apoptosis. Dimethylenastron activates the PI3K/Akt pathway, which in turn causes transcriptional up-regulation of Hsp70.
References
Certificates
Categories
Extra info
M. Gartner et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7.
M. Liu et al. Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells. J Biol Chem. 2006 Jun 30;281(26):18090-7.
M. Liu et al. Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor. Biochem Pharmacol. 2008 Jul 15;76(2):169-78.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
PI3K-Akt-mTOR
EC 3.6.4.4
KSP
Specific potent and cell-permeable inhibitor of Eg5 (KSP)
Chemical name
4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-1,2,3,4,7,8-hexahydroquinazolin-5(6H)-one
Parent CAS No.
[863774-58-7]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| P 505-15 - PRT 062607 | Axon 1936
CAS [1370261-96-3]
MF C19H23N9OMW 393.45
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Highly specific and potent inhibitor of spleen tyrosine kinase (Syk) (IC50: 1-2 nM)
References
Certificates
Categories
Extra info
G Coffey et al. Specific Inhibition of Spleen Tyrosine Kinase Suppresses Leukocyte Immune Function and Inflammation in Animal Models of Rheumatoid Arthritis. J. Pharmacol. Exp. Ther. 2012, 340(2), 350-359.
J Hoellenriegel et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Spleen tyrosine kinase (Syk)
EC 2.7.10.2
Inhibitor of spleen tyrosine kinase (Syk)
Chemical name
4-(3-(2H-1,2,3-triazol-2-yl)phenylamino)-2-((1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide
Parent CAS No.
[1370261-96-3]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Ispinesib - SB 715992 | Axon 2446
CAS [336113-53-2]
MF C30H33ClN4O2MW 517.06
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
The first potent, highly specific small-molecule inhibitor of the human kinesin spindle protein (KSP or KIF11 or Eg5), that induces mitosis-phase (M-phase) arrest followed by apoptosis in either the M-phase (via mitotic catastrophe) or G1-phase of the cell-cycle. Ispinesib alters the ability of KSP to bind to microtubules and inhibits its movement by preventing the release of ADP without preventing the release of the KSP−ADP complex from the microtubule
References
Certificates
Categories
Extra info
J.P. Holland et al. Fluorinated quinazolinones as potential radiotracers for imaging kinesin spindle protein expression. Bioorg Med Chem. 2013 Jan 15;21(2):496-507.
L. Lad et al. Mechanism of inhibition of human KSP by ispinesib. Biochemistry. 2008 Mar 18;47(11):3576-85.
L. Luo et al. ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism. Nat Chem Biol. 2007 Nov;3(11):722-6.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
EC 3.6.4.4
KSP
First potent, highly specific small-molecule inhibitor of human KSP
Chemical name
(R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)-4-methylbenzamide
Parent CAS No.
[336113-53-2]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| R 406 | Axon 1674
CAS [841290-80-0]
MF C22H23FN6O5MW 470.45
Purity:
98%
Soluble in DMSO
Description
Orally bioavailable and selective inhibitor of spleen tyrosine kinase (Syk) (Ki=30 nM). Active component of its prodrug R788 or R935788 (Fostamatinib)
References
Certificates
Categories
Extra info
S Braselmann et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J. Pharmacol. Exp. Ther. 2006, 319(3), 998-1008.
HS Cha et al. A Novel Spleen Tyrosine Kinase Inhibitor Blocks c-Jun N-Terminal Kinase-Mediated Gene Expression in Synoviocytes. J. Pharmacol. Exp. Ther. 2006, 317(2), 571-578.
JC Spalton et al. The novel Syk inhibitor R406 reveals mechanistic differences in the initiation of GPVI and CLEC-2 signaling in platelets. J. Thromb. Haemost. 2009, 7, 1-8.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Spleen tyrosine kinase (Syk)
EC 2.7.10.2
Spleen tyrosine kinase Inhibitor
Chemical name
6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
Parent CAS No.
[841290-80-0]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Suprafenacine - SRF | Axon 2398
CAS [1477482-50-0]
MF C16H18N4OMW 282.34
Purity:
99%
Soluble in DMSO
Description
Destabilizer of microtubules (IC50 value 0.38 µM for microtubule polymerization inhibition) that causes cell cycle arrest in the G2/M phase and cell death by apoptosis. Suprafenacine (SRF) was found to selectively inhibit cancer cell proliferation (IC50 values 83 - 381 nM in various cancer cell lines) and was effective against drug-resistant cancer cells by virtue of its ability to bypass the multidrug resistance transporter P-glycoprotein (P-gp).
References
Certificates
Categories
Extra info
B.H. Choi et al. Suprafenacine, an indazole-hydrazide agent, targets cancer cells through microtubule destabilization. PLoS One. 2014 Oct 29;9(10):e110955.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Tubulin
Destabilizer of microtubules that causes cell cycle arrest in the G2/M phase
Chemical name
(E)-N'-(4-methylbenzylidene)-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide
Parent CAS No.
[1477482-50-0]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| SPL-B - Spindlactone B | Axon 2474
CAS [1465248-60-5]
MF C27H22N2O5MW 454.47
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally active inhibitor of transforming acidic coiled-coil protein (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells, without affecting spindle assembly in normal cells. SPL significantly inhibits mitosis in cancer cells and suppresses in vivo tumor growth.
KEYWORDS: SPL-B | supplier | TACC3 inhibitor | Spindlactone B | SPLB | CAS [1465248-60-5] | microtubules | MTs | TACC | Inhibitor | proteins | mitotic spindle | assembly | mitosis | centrosomal | TOGp | Aurora A | coumarin | cell-cycle regulation | differentiation | | axonmedchem |
| IMM 01 | Axon 2406
CAS [218795-74-5]
MF C12H17N3O2SMW 267.35
Purity:
99%
Soluble in DMSO
Description
Small-molecule agonist of mammalian Diaphanous (mDia)-related formins that inhibited DID–DAD binding (IC50 value 140 nM). IMM-01 induced filopodia-like structures similar to those observed in cells expressing constitutively active mDia1 or mDia2. Moreover, IMM01 triggered actin assembly and microtubule stabilization consistent with formin activation in NIH 3T3 cells.
References
Certificates
Categories
Extra info
L.L. Lash et al. Small-molecule intramimics of formin autoinhibition: a new strategy to target the cytoskeletal remodeling machinery in cancer cells. Cancer Res. 2013 Nov 15;73(22):6793-803.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Immunology
mDia
Small-molecule agonist of mammalian Diaphanous (mDia)-related formins
Chemical name
N-tert-butyl-2-(2,4-dihydroxybenzylidene)hydrazinecarbothioamide
Parent CAS No.
[218795-74-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| BTB 1 - NSC 156750 | NSC 658180 | Axon 2407
CAS [86030-08-2]
MF C12H8ClNO4SMW 297.71
Purity:
99%
Soluble in DMSO and Ethanol
Description
The first small molecule reversible inhibitor of the mitotic motor protein Kif18A (IC50 value 1.69 µM for inhibition of Kif18A ATPase activity) that acts in an ATP-competitive and microtubule (Mt) uncompetitive manner.
BTB-1 (aka NSC 156750 or NSC 658180) was previously tested and found to inhibit HIV-1 replication (IC50 value 29.2 µM in cellular anti-HIV-1 assay), yet BTB1 proved to be cytotoxic at low micromolar concentrations.
References
Certificates
Categories
Extra info
J. Braun et al. Synthesis and Biological Evaluation of Optimized Inhibitors of the Mitotic Kinesin Kif18A. ACS Chem Biol. 2015 Feb 20;10(2):554-60.
M. Catarinella et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6.
N. Neamati et al. Diarylsulfones, a novel class of human immunodeficiency virus type 1 integrase inhibitors. Antimicrob Agents Chemother. 1997 Feb;41(2):385-93.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Kif18A
EC 3.6.4.4
The first small molecule reversible inhibitor of the mitotic motor protein Kif18A
Chemical name
4-chloro-2-nitro-1-(phenylsulfonyl)benzene
Parent CAS No.
[86030-08-2]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| KHS101 hydrochloride | Axon 2901
CAS [1784282-12-7]
MF C18H21N5S.HClMW 375.92
Purity:
99%
Soluble in water and DMSO
Description
KHS101 hydrochloride is a brain-penetrable TACC3 inhibitor known to enhance neuronal differentiation (EC50 value of 1 μM in cultured rat NPCs) and inhibit cell cycle progression and proliferation. KHS101 hydrochloride works indirectly on HIF complex formation by destabilizing both TACC3 and the HIF component HIF-1α. KHS101 hydrochloride suppresses proliferation, migration, and invasive capabilities of breast cancer cells, EMT process, and mammosphere forming capability, alters cell cycle progression, and induces apoptosis.
KEYWORDS: SKHS101 hydrochloride | supplier | TACC3 inhibitor | KHS 101 hydrochloride | KHS-101 hydrochloride | CAS [1784282-12-7] | [1262770-73-9] | Microtubules | TACC | Inhibitor | Proteins | TACC3 | NPC | HIF | HIF-1α | Breast cancer | | axonmedchem |
| Remodelin | Axon 2299
CAS [949912-58-7]
MF C15H14N4SMW 282.36
Purity:
99%
Soluble in DMSO
Description
Potent Acetyl-transferase NAT 10 inhibitor that mediates nuclear shape rescue in laminopathic (LMNA-depleted) cells via microtubule reorganization. Remodelin markedly reduced the prevalence of misshapen nuclei in HGPS cells as well as in primary MRC5 fibroblasts aged in culture. In contrast, Remodelin had no effect on nonlaminopathic Werner syndrome cells
References
Certificates
Categories
Extra info
D. Larrieu et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014, 344, 527-532.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
NAT 10
EC 2.3.1.
Potent NAT 10 inhibitor that mediates nuclear shape rescue in laminopathic cells via microtubule reorganization
Chemical name
4-(2-(2-cyclopentylidenehydrazinyl)thiazol-4-yl)benzonitrile
Parent CAS No.
[949912-58-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Cenicriviroc - TBR 652 | TAK 652 | CVC | Axon 2665
CAS [497223-25-3]
MF C41H52N4O4SMW 696.94
Purity:
99%
Soluble in DMSO
Description
Oral CCR5-antagonist for treatment of HIV infection (IC50 value 0.043 nM for the wild-type virus (KKWT) was in PBMCs) that also has activity against the inflammatory chemokine CCR2.
KEYWORDS: Cenicriviroc | supplier | CCR5 antagonist | TBR 652 | TAK 652 | CVC | TBR652 | TAK652 | CAS [497223-25-3] | [497223-28-6] | Chemokine | GPCR | CCR2 | HIV-1 | viral replication | antiretroviral | inflammatory | gp120 | | axonmedchem |
| WX-132-18B | Axon 2816
CAS [1415262-07-5]
MF C18H16N4O2MW 320.35
Purity:
99%
Soluble in DMSO
Description
WX-132-18B is a microtubule-depolymerizing agent that selectively acts on the colchicine-binding site of tubulin and exerts potent in vitro and in vivo anti-tumor effects. Specifically, WX-132-18B exhibited high in vitro cytotoxic activity (GI50 value of 1.9–3.2 nM), significant potency against tubulin assembly (IC50 value of 0.77 μM), and substantial inhibition of colchicine binding (99% at 5 μM). Moreover, WX-132-18B caused cell arrest in G2/M phase.
KEYWORDS: WX-132-18B | Supplier | Microtubule inhibitor | WX132-18B | WX 132-18B | CAS [1415262-07-5] | Cytoskeleton | Tubulin | Inhibitor | Proteins | Colchicine | G2/M phase | | axonmedchem |
| Neuropathiazol | Axon 2322
CAS [880090-88-0]
MF C19H18N2O2SMW 338.42
Purity:
99%
Soluble in DMSO
Description
Selective inducer of neural differentiation of adult hippocampal neural progenitor cells (NPCs). Neuropathiazole competitively suppresses astrogliogenesis by LIF/BMP2/FBS in a dose-dependent manner. Useful tool for studying the molecular mechanisms that determine cell fate with the ultimate goal of stem-cell therapy.
References
Certificates
Categories
Extra info
M. Warashina et al. A synthetic small molecule that induces neuronal differentiation of adult hippocampal neural progenitor cells. Angew. Chem. Int. Ed. Engl. 2006, 45, 591-593.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Stem Cell
Stem Cell Differentiator
Selective inducer of neural differentiation of adult hippocampal neural progenitor cells (NPCs).
Chemical name
ethyl 4-(methyl(2-phenylthiazol-4-yl)amino)benzoate
Parent CAS No.
[880090-88-0]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Gallic acid - NSC 674319 | Axon 2208
CAS [149-91-7]
MF C7H6O5MW 170.12
Purity:
100%
Soluble in water and DMSO
Description
Multi-affinity drug. Targets Carbonic Anhydrases, FUT7, P4H, HATs, among many others in an inhibitory modus. Gallic acid is cytotoxic to cancer cells and has anti-inflammatory and antioxidative effects. Gallic acid was found to inhibit the histone acetyltransferase activity of several HATs (IC50 values: 14, 24, 25 and 34 μM for p300, CBP, Tip60 and PCAF respectively). In particular, it inhibited p300/CBP-dependent HAT activities uncompetitively, while being devoid of activity towards other epigenetic enzymes including SIRT1, HDAC, and HMTase. In A549 lung cancer cells, Gallic acid inhibited the acetylation of p65, leading to the downregulation of NF-κB activation in response to diverse inflammatory signals.Gallic acid is also known to inhibit HIV-1 infections through inhibition of HIV-1 reverse transcriptase activity in Lagerstroemia speciosa L.
References
Certificates
Categories
Extra info
A. Innocenti et al. Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I–XIV with a series of natural product polyphenols and phenolic acids. Bioorg. Med. Chem. 2010, 18, 2159–2164.
K.C. Choi. Gallic acid suppresses lipopolysaccharide-induced nuclear factor-kappaB signaling by preventing RelA acetylation in A549 lung cancer cells. Mol. Cancer Res. 2009, 12, 2011-2021.
K. Majamaa et al. Partial identity of the 2-oxoglutarate and ascorbate binding sites of prolyl 4-hydroxylase. J. Biol. Chem. 1986, 261, 7819-7823.
S. Madlener et al. Gallic acid inhibits ribonucleotide reductase and cyclooxygenases in human HL-60 promyelocytic leukemia cells. Cancer. Lett. 2007, 245, 156–162.
X. Niu et al. Inhibition of fucosyltransferase VII by gallic acid and its derivatives. Arch. Biochem. Biophys. 2004, 425, 51-57.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
Carbonic Anhydrase
HAT
RT
NF-κB
EC 2.3.1.48
Multi-affinity drug. Antioxidant.
Chemical name
3,4,5-trihydroxybenzoic acid
Parent CAS No.
[149-91-7]
Order
Size
Unit Price
Stock
100 mg
€50.00
In Stock | | axonmedchem |
| LIT-927 | Axon 2921
CAS [2172879-52-4]
MF C17H13ClN2O3MW 328.75
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
LIT-927 is a selective, locally and orally active CXCL12 neutraligand (Ki value of 267 nM). Moreover, LIT-927 shows an anti-inflammatory effect in a murine model of allergic airway hypereosinophilia.
KEYWORDS: LIT-927 | supplier | CXCL12 neutraligand | LIT927 | LIT 927 | CAS [2172879-52-4] | Chemokine | Chemokine | Neutraligand | Receptors | Hypereosinophilia | CXCR4 | | axonmedchem |
| SP-6-27 | Axon 2815
CAS [1384170-58-4]
MF C24H24N4OMW 384.47
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
The microtubule inhibitor SP-6-27 inhibits angiogenesis and induces apoptosis in ovarian cancer cells. Moreover, SP-6-27 is active against four human glioma cell lines (T98, U87, LN18, A172) and particularly against the A172 glioma cell line (IC50 value of 7.4 nM).
KEYWORDS: SP-6-27 | supplier | Microtubule inhibitor | SP6-27 | SP 6-27 | CAS [1384170-58-4] | Cytoskeleton | Tubulin | Inhibitor | Proteins | Apoptosis | Ovarian Cancer | A172 | Glioma Cells | | axonmedchem |
| FPH 2 - BRD 9424 | Axon 2355
CAS [957485-64-2]
MF C14H16ClN5O2SMW 353.83
Purity:
99%
Soluble in DMSO
Description
Small molecule that concentration dependently induces proliferation and enhances the functions of mature human primary hepatocytes. Over 7 days, FPH 2 induced hepatocyte doublings at a rate that is consistent with reported liver regeneration kinetics in vivo.
References
Certificates
Categories
Extra info
J. Shan et al. Identification of small molecules for human hepatocyte expansion and iPS differentiation. Nat. Chem. Biol. 2013, 9, 514-520.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Diabetes & Metabolism
Stem Cell
Stem Cell Differentiator
Proliferation inducer of mature human primary hepatocytes
Chemical name
4-(3-(5-chloro-2-methoxyphenyl)thioureido)-1-ethyl-1H-pyrazole-3-carboxamide
Parent CAS No.
[957485-64-2]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Dolutegravir - GSK 1349572 | Soltegravir | Tivicay | Axon 2855
CAS [1051375-16-6]
MF C20H19F2N3O5MW 419.38
Purity:
99%
Soluble in DMSO
Description
Dolutegravir is an HIV integrase inhibitor with potent in vitro anti-HIV activity (IC50 value of 0.51 nM), an in vitro resistance profile different from those of other integrase inhibitors, and favorable preclinical safety and pharmacokinetics.
KEYWORDS: Dolutegravir | supplier | HIV integrase inhibitor | GSK 1349572 | Soltegravir | Tivicay | GSK1349572 | GSK-1349572 | CAS [1051375-16-6] | DNA | HIV | Inhibitor | Enzymes | | axonmedchem |
| AZD 8797 - CX3CR1 antagonist 18a | Axon 2255
CAS [911715-90-7]
MF C19H25N5OS2MW 403.56
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective antagonist of the Fractalkine receptor (FKN or CX3CR1; Ki value 3.9 nM) with a 720 fold selectivity over the CXCR2 receptor, a 246-fold selectivity versus hCCR1 and 187-fold versus hCCR2 and no significant antagonism of the CCR4, CCR5, CCR6, CXCR3, and CXCR5 receptors. AZD 8797 displayed adequate metabolic stability and solubility and high Caco-2 permeability. Notably, AZD 8797 exhibited a significant interaction (>50% activity at 10 μM) for the adenosine A1 receptor only, and the selectivity was later determined to be 33-fold.
KEYWORDS: | | axonmedchem |
| Cardiogenol C hydrochloride | Axon 2550
CAS [1049741-55-0]
MF C13H16N4O2.HClMW 296.75
Purity:
99%
Soluble in water and DMSO
Description
Selective and efficient inducer of the differentiation of ESCs to cardiomyocytes (EC50 value 0.1 µM for inducing the differentiation of myosin heavy chain (MHC) positive cardiomyocytes from ESCs in P19CL6 cells). Cardiogenol C induces cardiomyogenic function in lineage-committed progenitor cells, and can thus be considered a promising tool to improve cardiac repair by cell therapy.
KEYWORDS: Cardiogenol C | supplier | Stem cell differentiator | CAS [671225-39-1] | [1049741-55-0] | Stem cells (iPSC) | Modulator | differentiation | ESCs | cardiomyocytes | myosin heavy chain |MHC| cardiac repair | | axonmedchem |
| BMH 21 | Axon 2462
CAS [896705-16-1]
MF C21H20N4O2MW 360.41
Purity:
99%
Soluble in 0.1N HCl (aq)
Description
RNA polymerase I (RNAP1) inhibitor (IC50 values 0.05 µM and 0.07 µM for degradation of RPA194 and translocation of NCL, respectively). BMH-21 intercalates with GC-rich rDNA, inhibits Pol I, and causes activation of p53 and proteasome-mediated degradation of RPA194. Furthermore, BMH21 showed broad and potent anticancer activity in NCI60 cancer cell lines and reduced tumor burden in mouse xenograft assays.
References
Certificates
Categories
Extra info
L. Colis et al.Design, synthesis, and structure-activity relationships of pyridoquinazolinecarboxamides as RNA polymerase I inhibitors. J Med Chem. 2014 Jun 12;57(11):4950-61.
K. Peltonen et al. Identification of novel p53 pathway activating small-molecule compounds reveals unexpected similarities with known therapeutic agents. PLoS One. 2010 Sep 27;5(9):e12996.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Immunology
RNAP1
p53-Tumor Suppression
DNA-damage Response
EC 2.7.7.6
Inhibitor of RNA Polymerase I (RNAP1)
Chemical name
N-(2-(dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
Parent CAS No.
[896705-16-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| YJC-10592 | Axon 2636
CAS [1226894-87-6]
MF C27H31ClF3N5O3MW 566.01
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
YJC-10592 is a CC chemokine receptor 2 (CCR2) antagonist (IC50 value 1.12 μM), which also showed excellent inhibitory activity in the calcium assay (IC50 value 1.7 nM), and good potency in the chemotaxis assay (IC50 value 23 nM). In rats, YJC-10592 showed dose-dependent pharmacokinetics and low F value due to slower elimination and incomplete absorption.
KEYWORDS: YJC-10592 | supplier | CCR2 antagonist | YJC10592 | YJC 10592 | CAS [1226894-87-6] | Chemokine | Antagonist | Receptors | CCR2 | CCR 2 | | axonmedchem |
| CX 5461 | Axon 2173
CAS [1138549-36-6]
MF C27H27N7O2SMW 513.61
Purity:
99%
Soluble in 0.1N HCl(aq)
Description
First selective inhibitor of RNA Polymerase I (Pol I or RNAP1, IC50 of 0.88 μM) transcription with in vivo activity in tumor growth efficacy models; potent and orally bioavailable. CX 5461 demonstrated approximately 200-fold selectivity against Pol I relative to Pol II. It selectively kills tumor cells by activating p53-dependent apoptosis. It also shows potent antiproliferative capacity in human hematologic tumor cells.
References
Certificates
Categories
Extra info
M. Haddach et al. Discovery of CX-5461, the first direct and selective inhibitor of RNA Polymerase I, for cancer therapeutics. ACS Med. Chem. Lett. 2012, 3, 602-606.
M.J. Bywater et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell 2012, 22, 51-65.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Immunology
RNAP1
p53-Tumor Suppression
DNA-damage Response
EC 2.7.7.6
Inhibitor of RNA Polymerase I (RNAP1)
Chemical name
2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-Benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
Parent CAS No.
[1138549-36-6]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| BX 471 | Axon 2082
CAS [217645-70-0]
MF C21H24ClFN4O3MW 434.89
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
Potent, orally active and selective chemokine receptor CCR1 antagonist
References
Certificates
Categories
Extra info
M Liang et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J. Biol. Chem. 2000, 275(25), 19000.
N Vaidehi et al. Predictions of CCR1 chemokine receptor structure and BX 471 antagonist binding followed by experimental validation. J. Biol. Chem. 2006, 281(37), 27613-27620.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
A1
Chemokine
Selective CCR1 receptor antagonist
Chemical name
(R)-1-(5-chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea
Parent CAS No.
[217645-70-0]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| EML 425 | Axon 2568
CAS [1675821-32-5]
MF C27H24N2O4MW 440.49
Purity:
99%
Soluble in DMSO
Description
Potent, selective and cell permeable reversible dual inhibitor of CBP and p300 (IC50 values 1.1 μM and 2.9 μM, respectively, and practically inactive against the enzymes GCN5 and PCAF), noncompetitive versus both acetyl-CoA and a histone H3 peptide. EML425 induced a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9, a marked arrest in the G0/G1 phase and a significant increase in the hypodiploid nuclei percentage in human leukemia U937 cells. EML425's potency is comparable to that of C646 (Axon 1781).
KEYWORDS: EML 425 | supplier | dual CBP/p300 KAT3 inhibitor | EML425 | CAS [1675821-32-5] | Histone | HAT | Inhibitor | Lysine acyltransferase | H4K5 | H3K9 | G0/G1 arrest | hypodiploid nuclei | C646 | | axonmedchem |
| TH 1834 | Axon 2339
CAS [N.A.]
MF C33H40N6O3.2HClMW 641.63
Purity:
99%
Soluble in water and DMSO
Description
Tip60 histone acetyltransferase inhibitor. Treating cells with TH1834 results in apoptosis and increased unrepaired DNA damage (following ionizing radiation treatment) in breast cancer but not control cell lines. Furthermore, TH 1834 did not affect the activity of related HAT MOF, as indicated by H4K16Ac, demonstrating specificity.
References
Certificates
Categories
Extra info
C. Gao et al. Rational design and validation of a Tip60 histone acetyltransferase inhibitor. Sci. Rep. 2014, 4, 5372.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
HAT
Transcription Factors
p53-Tumor Suppression
Wnt-β-Catenin
NF-κB
JAK-STAT
DNA-damage Response
EC 2.3.1.48
Tip60 histone acetyltransferase inhibitor
Chemical name
2-(5-(4-((phenethyl(4-(4-(pyrrolidin-1-ylmethyl)phenoxy)butyl)amino)methyl)phenyl)-2H-tetrazol-2-yl)acetic acid dihydrochloride
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| FH 1 - NSC 12407 | BRD K4477 | Axon 2320
CAS [2719-05-3]
MF C17H18N2O2MW 282.34
Purity:
99%
Soluble in DMSO
Description
Promotes the maturation and differentiation of induced pluripontent stem cells (iPSCs) to hepatocytes. FH 1 treatment augmented albumin levels and the expression levels of ABCB11 in iHEP cells.
References
Certificates
Categories
Extra info
J. Shan et al. Identification of small molecules for human hepatocyte expansion and iPS differentiation. Nat. Chem. Biol. 2013, 9, 514-520.
Certificate of Analysis
Material Safety Data Sheet
Stem Cell
Stem Cell Differentiator
Promotes the maturation and differentiation of iPSCs to hepatocytes
Chemical name
N,N'-(4,4'-methylenebis(4,1-phenylene))diacetamide
Parent CAS No.
[2719-05-3]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| CPTH2 | Axon 2765
CAS [357649-93-5]
MF C14H14ClN3SMW 291.80
Purity:
100%
Soluble in DMSO
Description
CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating Gcn5p network in vitro and in vivo.
KEYWORDS: CPTH2 | supplier | HAT inhibitor | CPTH-2 | CPTH 2 | CAS [357649-93-5] | Histone | HAT | Inhibitor | Enzymes | Gcn5 | Gcn5p | | axonmedchem |
| MPT0B098 | Axon 2658
CAS [1254363-89-7]
MF C20H18N2O3SMW 366.43
Purity:
99%
Soluble in DMSO
Description
Microtubule inhibitor that binds to the colchicine-binding site of tubulin and suppresses JAK2/STAT3 signaling pathway through modulation of SOCS3 stability. MPT0B098 arrests cells in the G2-M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA.
KEYWORDS: MPT0B098 | supplier | Microtubule inhibitor | CAS [1254363-89-7] | Cytoskeleton | Tubulin | Inhibitor | colchicine | JAK2/STAT3 | SOCS3 | cell arrest | G2-M | apoptosis | cell migration | HIF-1α | | axonmedchem |
| AZD 2098 | Axon 2842
CAS [566203-88-1]
MF C11H9Cl2N3O3SMW 334.18
Purity:
99%
Soluble in DMSO
Description
Potent, selective and bioavailable CCR4 receptor antagonist (pIC50 value of 7.8).
KEYWORDS: AZD 2098 | supplier | CCR4 antagonist | AZD2098 | AZD-2098 | CAS [566203-88-1] | Chemokine | Chemokine | Antagonist | Receptors | | axonmedchem |
| ZK 756326 dihydrochloride | Axon 2861
CAS [1780259-94-0]
MF C21H28N2O3.2HClMW 429.38
Purity:
98%
Soluble in water and DMSO
Description
ZK 756326 dihydrochloride is a nonpeptide chemokine CCR8 receptor agonist (IC50 value of 1.8 μM). This compound may be useful in evaluating the physiological role of CCR8 in HIV infection, as well as in the general study of CCR8 biology without the constraints inherent to the use of protein agonists such as its natural ligand.
KEYWORDS: ZK 756326 dihydrochloride | supplier | CCR8 agonist | ZK756326 dihydrochloride | ZK-756326 dihydrochloride | CAS [1780259-94-0] | [874911-96-3] | Chemokine | Agonist | Receptors | HIV | | axonmedchem |
| L 002 - NSC 764414 | Axon 2319
CAS [321695-57-2]
MF C15H15NO5SMW 321.35
Purity:
99%
Soluble in DMSO
Description
Inhibitor of p300 histone acyltransferase (a.k.a KAT3B; IC50 value 1.98 μM in vitro) that also inhibited acetylation of histones and p53, and suppresses STAT3 activation in cell-based assays. In vivo, L 002 potently suppressed tumor growth of TNBC cell line MDA-MB-468 xenografts.
References
Certificates
Categories
Extra info
H. Yang et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol. Cancer Ther. 2013, 12, 610-620.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
HAT
p53
Transcription Factors
p53-Tumor Suppression
NF-κB
JAK-STAT
EC 2.3.1.48
Inhibitor of p300 HAT (KAT3B) and p53 acetylation
Chemical name
4-(4-methoxyphenylsulfonyloxyimino)-2,6-dimethylcyclohexa-2,5-dienone
Parent CAS No.
[321695-57-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |