GSK-481( GSK481 | GSK'481 )

Catalog No. M12392 CAS No. 1622849-58-4

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Product Name

GSK-481
Note

Research use only, not for human use.
Brief Description

A highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM.
Description

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.
In Vitro

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.
In Vivo

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

GSK481 | GSK'481
Pathway

Apoptosis
Target

RIP kinase
Recptor

RIP1
Research Area

Cancer
Indication

——

CAS Number

1622849-58-4
Formula Weight

377.3932
Molecular Formula

C21H19N3O4
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 35 mg/mL
SMILES

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

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

1. Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78.

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