GSK481

GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM) . GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM[1].

Product Specifications

CAS Number

[1622849-58-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

RIP kinase

Type

Reference compound

Related Pathways

Apoptosis

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/GSK_acute_481.html

Concentration

10mM

Purity

98.04

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

Molecular Formula

C21H19N3O4

Molecular Weight

377.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59 (5) :2163-78.|[2]Lee HL, et al. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66.