A RIPK1 inhibitor (IC50s = 16 and 2

GSK2982772 – 1 mg

Brand:
Cayman
CAS:
1622848-92-3
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively).{49425} It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.  

 

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SKU: 29230 - 1 mg Category:

Description

A RIPK1 inhibitor (IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively); >10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM; inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively); decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis at 3-300 nM; increases survival in a mouse model of TNF-α-induced lethal shock at 3, 10, and 50 mg/kg

Formal name: 3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide

Synonyms: 

Molecular weight: 377.4

CAS: 1622848-92-3

Purity: ≥98%

Formulation: A solid

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