A selective p38α/β MAPK inhibitor (pKi = 8.1 and 7.6

GW 856553X – 10 mg

Brand:
Cayman
CAS:
585543-15-3
Storage:
-20
UN-No:
Non-Hazardous - /

GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}  

 

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Description

A selective p38α/β MAPK inhibitor (pKi = 8.1 and 7.6, respectively); inhibits TNF-α production (IC50 = 31 nM); improves survival and blood pressure in hypertensive rats; did not proceed past Phase II clinical trials,,

Formal name: 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide

Synonyms:  GSK-AHAB|SB 856553

Molecular weight: 383.5

CAS: 585543-15-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Cell Biology|Cell Signaling|p38 MAPK Signaling||Research Area|Immunology & Inflammation|Innate Immunity

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