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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 µ,M for c-Fyn, 4.3 nM for I338G, v-src-as1 vs. 28 µ,M for v-src, 5 nM for F80G, CDK2-as1 vs. 29 µ,M for CDK2, 8 nM for F89G, CAMK IIa-as1 vs. 24 µ,M for CAMKII, 120 nM for T315A, c-Abl-as2 vs. 3.4 µ,M 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 µ,M for c-Fyn, 4.3 nM for I338G, v-src-as1 vs. 28 µ,M for v-src, 5 nM for F80G, CDK2-as1 vs. 29 µ,M for CDK2, 8 nM for F89G, CAMK IIa-as1 vs. 24 µ,M for CAMKII, 120 nM for T315A, c-Abl-as2 vs. 3.4 µ,M for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase.