InSolution K-252a; Nocardiopsis sp.

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetCaM kinase II

Target K_i: 1.8 nM, 20 nM, 18 nM, 25 nM, 20 nM, 3 nM, against CaM kinase II, myosin light chain kinase, protein kinase A, protein kinase C, protein kinase G, NGF receptor gp140trk, respectively

Cell permeable: yes

General description

A cell-permeable protein kinase inhibitor that inhibits CaM kinase II (K_i = 1.8 nM), myosin light chain kinase (K_i = 17 nM), protein kinase A (K_i = 18 nM), protein kinase C (K_i = 25 nM), and protein kinase G (K_i = 20 nM). Also acts as a potent inhibitor (IC₅₀ = 3 nM) of the tyrosine protein kinase activity of the NGF receptor gp 140trk, the product of the trk protooncogene. Also inhibits the kinase activity of its transforming alleles, the trk oncogenes, and of the related neurotrophin receptors gp 145trkB and gp 145trkC. Induces apoptosis and cell cycle arrest by inhibiting Cdc2 and Cdc25c.

Legal Information

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

Other Notes

Chin, L.S., et al. 1999. Cancer Invest.17, 391.Nakanishi, N., et al. 1995. FEBS Lett.368, 411.Ross, A.H., et al. 1995. J. Neurochem.65, 2748.Mizuno, K., et al. 1993. FEBS Lett.330, 114.Pawlowska, Z., et al. 1993. J. Neurochem.60, 678.Tapley, P., et al. 1992. Oncogene7, 371.Simpson, D.L., et al. 1991. J. Neurosci. Res.28, 486.Hashimoto, S. 1988. J. Cell Biol.107, 1531.Koizuma, S., et al. 1988. J. Neurosci.8, 715.Kase, H., et al. 1987. Biochem. Biophys. Res. Commun.142, 436.

Packaging

Packaged under inert gas

100 µg in Plastic ampoule

Physical form

A 1 mM (100 µg/214 µl) solution of K-252a (Cat. No. 420298) in DMSO.

Reconstitution

Following initial thaw aliquot and freeze at (-20°C). Store under an inert atmosphere.

Warning

Toxicity: Irritant (B)