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VX-702

Catalog No. T2513 CAS 745833-23-2

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

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VX-702, CAS 745833-23-2

Pack Size	Availability	Price/USD
10 mg	In stock	$ 50.00
25 mg	In stock	$ 77.00
50 mg	In stock	$ 135.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 100%

Purity: 99%

Purity: 98.96%

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Description	VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).
Targets&IC50	p38α:4 nM-20 nM
In vitro	Administering VX-702 (0.1 mg/kg) twice daily exhibited effects similar to those of methotrexate (0.1 mg/kg). Furthermore, the efficacy of administering VX-702 (5 mg/kg) twice daily was akin to that of a once-daily dose of prednisolone (10 mg/kg). The MI/AAR ratio in the group treated with VX-702 (50 mg/kg) was significantly lower compared to both the control group and the group treated with VX-702 at 5 mg/kg. VX-702 has a half-life of 16-20 hours, a clearance volume of 3.75 L, and a distribution volume of 73 L/kg. It selectively inhibits the activity of p38 MAPK without affecting ERKs and JNKs.
In vivo	VX-702 does not inhibit platelet aggregation induced by p38 MAPK activators. Treatment with VX-702 (1 μM) can completely or partially suppress p38 activity induced by various platelet activators, including thrombin, AYPGKF, SFLLRN, U46619, and collagen, with an IC50 ranging from 4-20 nM. Additionally, VX-702 dose-dependently inhibits the production of IL-6 (IC50: 59 ng/ml), IL-1β (IC50: 122 ng/ml), and TNFα (IC50: 99 ng/ml).
Kinase Assay	HDAC enzyme assay in vitro: The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.

Molecular Weight	404.32
Formula	C19H12F4N4O2
CAS No.	745833-23-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 75 mg/mL (185.5 mM)

References and Literature

1. Kuliopulos A, et al. Thromb Haemost, 2004, 92(6), 1387-1393. 2. Braddock M, IDDB Meeting Report, 2005, March 14-15. 3. Gill A, IDDB Meeing Report, 2002, March 06-08. 4. Bhattacharya K, et al. Circulation, 2003, 108(17), 882.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Liver Cancer Compound Library Bioactive Compounds Library Max NO PAINS Compound Library MAPK Inhibitor Library Apoptosis Compound Library Pyroptosis Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

VX-702 745833-23-2 Autophagy MAPK p38 MAPK Inhibitor inhibit VX702 VX 702 inhibitor

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