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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-GSK3145095
GSK3145095

Chemical Structure : GSK3145095

CAS No.: 1622849-43-7

GSK3145095 (GSK 3145095)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 397.386
分子式 C20H17F2N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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