[CAS NO. 2049868-46-2]  GSK'963

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PRODUCTS SPECIFICATIONS [2049868-46-2]

Catalog
SLK-S8642
Brand
Selleck
CAS
2049868-46-2

DESCRIPTION [2049868-46-2]

Overview

MDL-
Molecular Weight230.31
Molecular FormulaC14H18N2O
SMILESCC(C)(C)C(N1N=CC[C@H]1C2=CC=CC=C2)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM4.3420 mL21.7099 mL43.4197 mL
5 mM0.8684 mL4.3420 mL8.6839 mL
10 mM0.4342 mL2.1710 mL4.3420 mL
50 mM0.0868 mL0.4342 mL0.8684 mL

Description

GSK'963 is a chiral small-molecule inhibitor of with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

Targets

RIP1 kinase [1]
(Cell-free assay)
29 nM

In vitro

GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells.

In vivo

GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2 mg/kg, GSK'963 would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1.