GSK3145095

Research use only, not for human use.

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic. GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinase-dependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor was also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures. (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) .

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) .

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Apoptosis

TNF

RIP1

Endocrine system;Cancer

Neoplasms, Pancreatic

1622849-43-7

397.38

C20H17F2N5O2

>98% (HPLC)

DMSO:245mg/ml (616.54 Mm; Need ultrasonic)

FC1=CC2=C(NC(=O)[C@H](CC2)NC(=O)C2=NNC(CC3=CC=CC=C3)=N2)C(F)=C1

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(-20℃)

With Ice Pack

≥ 2 years