RIPK1 inhibitor GS3145095

Names

[ CAS No. ]:
1622849-43-7

[ Name ]:
RIPK1 inhibitor GS3145095

Biological Activity

[Description]:

GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM [1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> RIP kinase

[Target]

IC50: 6.3 nM (RIP1 kinase )[1]

[In Vitro]

GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM) [1].

[References]

[1]. Philip A. Harris, et al. Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. ACS Medicinal Chemistry Letters Article ASAP.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₇F₂N₅O₂

[ Molecular Weight ]:
397.38

RIPK1 inhibitor GS3145095

Names

Biological Activity

Chemical & Physical Properties

Related Compounds