InSolution K-252a, Nocardiopsis sp. - CAS 97161-97-2 - Calbiochem

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CaM kinase II

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

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.

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.

Legal Information

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