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GSK3145095

Chemical Structure : GSK3145095

CAS No.: 1622849-43-7

GSK3145095 (GSK 3145095)

Catalog No.: PC-72999Not For Human Use, Lab Use Only.

GSK3145095 (GSK 3145095) is a potent, selective RIP1 Kinase (RIPK1) inhibitor with IC50 of 6.3 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK3145095 (GSK 3145095) is a potent, selective RIP1 Kinase (RIPK1) inhibitor with IC50 of 6.3 nM.
GSK3145095 displays >1500-fold selectivity window at Reaction Biology Corp (359 kinases) and a competition binding assay KINOMEscan at DiscoveRx Corp (456 kinases).
GSK3145095 binds an allosteric pocket at the back of the ATP binding site.
Necroptosis pathway is activated through stimulation with TNF coincubated with the caspase inhibitor QVD-Oph or zVAD.fmk, and the SMAC mimetic RMT 5265, GSK3145095 is very potent as measured by inhibition of cytokine MIP-1β ((IC50=5 nM).
GSK3145095 promoted a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.

Physicochemical Properties

M.Wt 397.386
Formula C20H17F2N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-5-benzyl-N-(7,9-difluoro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-1H-1,2,4-triazole-3-carboxamide

References

1. Philip A Harris, et al. ACS Med Chem Lett. 2019 May 9;10(6):857-862.

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