Biochem/physiol Actions

Target IC₅₀: 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µ

Primary Targetmutant c-Fyn, v-src, Cadk2, CaMKIIa, c-Abl etc.,

Reversible: yes

Cell permeable: yes

General description

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 IIa-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.

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 IIa-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

Physical form

A 10 mM (1 mg/302 µL) solution of PP1 Analog II, 1NM-PP1 (Cat. No. 529581) in DMSO.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -70°C.

Warning

Toxicity: Irritant (B)