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Key Documents

420297

Sigma-Aldrich

K-252a, Nocardiopsis sp.

InSolution, ≥95%, A cell-permeable protein kinase inhibitor

Synonym(s):

InSolution K-252a, Nocardiopsis sp.

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About This Item

Empirical Formula (Hill Notation):
C27H21N3O5
CAS Number:
Molecular Weight:
467.47
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

shipped in

wet ice

storage temp.

−20°C

InChI

1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)

InChI key

KOZFSFOOLUUIGY-UHFFFAOYSA-N

General description

A cell-permeable protein kinase inhibitor that inhibits CaM kinase II (Ki = 1.8 nM), myosin light chain kinase (Ki = 17 nM), protein kinase A (Ki = 18 nM), protein kinase C (Ki = 25 nM), and protein kinase G (Ki = 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 Ki: 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

Storage Class Code

10 - Combustible liquids

WGK

WGK 1

Flash Point(F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Flash Point(C)

87 °C - closed cup - (Dimethylsulfoxide)


Certificates of Analysis (COA)

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