GSK-481

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、单激酶选择性和 ATP 竞争性的 RIP1 激酶抑制剂，生化 IC50 为 10 nM。

A highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM; displays complete specificity for RIP1 kinase over a panel of 456 kinases; exhibits excellent translation in the U937 cellular assay with IC50 of 10 nM, demonstrates significant blockage of the induced RIP1 autophosphorylation at Ser166 in HT29 cells; possesses good pharmacokinetic profiles in rodents.

GSK481 (300 nM; 2 hours; Jurkat cells) abrogates the RIP3 up-regulation induces by both TNFa and shikonin in live and dead cells, indicating that necroptosis is in fact induced by both agents. Apoptosis Analysis Cell Line:Jurkat cells Concentration:300 nM Incubation Time:2 hours Result:Increased levels of detectable apoptosis induced by TNFa and shikonin.

GSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse.

GSK481 | GSK'481

Apoptosis

RIP kinase

RIP1

Cancer

——

1622849-58-4

377.3932

C21H19N3O4

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O

3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-

(-20℃)

With Ice Pack

≥ 2 years