Biochem/physiol Actions
Target IC50: 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs.
Reversible: yes
Product competes with ATP.
Primary TargetT339G
Cell permeable: yes
General description
A cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent and selective ATP-competitive inhibitor of mutant kinases over wild-type (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase. Also available as a 10 mM solution in DMSO (Cat. No. 529606).
A cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases compared to the corresponding wild-type kinase (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Ira, G., et al. 2004. Nature431, 1011.Papa, F.R., et al. 2003. Science302, 1533.Bishop, A.C., et al. 2000. Nature407, 395.Weiss, E.L., et al. 2000. Nat. Cell Biol.2, 677.Bishop, A.C., et al. 1999. J. Am. Chem. Soc.121, 627.
Packaging
Packaged under inert gas
1 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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