A third generation inhibitor of p38 MAP kinases

VX-702 – 10 mg

Brand:
Cayman
CAS:
745833-23-2
Storage:
-20
UN-No:
Non-Hazardous - /

VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion.{21533} It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.{21533} VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.{21534} Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.{21532}  

 

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Description

A third generation inhibitor of p38 MAP kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively); inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively

Formal name: 6-[(aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide

Synonyms: 

Molecular weight: 404.3

CAS: 745833-23-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|p38 MAPK Signaling||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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