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Catalog:
SLK-S8642
Brand:
Selleck
CAS:
2049868-46-2
Overview
MDL
-
Molecular Weight
230.31
Molecular Formula
C14H18N2O
SMILES
CC(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 mg
5 mg
10 mg
1 mM
4.3420 mL
21.7099 mL
43.4197 mL
5 mM
0.8684 mL
4.3420 mL
8.6839 mL
10 mM
0.4342 mL
2.1710 mL
4.3420 mL
50 mM
0.0868 mL
0.4342 mL
0.8684 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.
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.
