PP1 Analog II, 1NM-PP1

A cell-permeable and reversible PP1 analog 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.

Cell permeable: yes

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

Reversible: yes

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

Packaged under inert gas

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

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

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Irritant (B)