GSK3145095 是一种 RIP1 激酶抑制剂，IC50 为 6.3 nM。
GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM [1].
IC50: 6.3 nM (RIP1 kinase )[1]
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].
Reference:
[1]. Harris PA, ET AL. Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. ACS Med Chem Lett. 2019 May 9;10(6):857-862.
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