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Key Documents

420298-M

Sigma-Aldrich

K-252a, Nocardiopsis sp.

A cell-permeable, reversible, and ATP-competitive inhibitor against multiple protein kinases.

Synonym(s):

K-252a, Nocardiopsis sp.

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About This Item

Empirical Formula (Hill Notation):
C27H21N3O5
CAS Number:
Molecular Weight:
467.47
UNSPSC Code:
12352202
NACRES:
NA.77

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 1 mg/mL
DMF: soluble

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, reversible, and ATP-competitive inhibitor against multiple protein kinases, including, but not limited to, CaM kinase II (Ki = 1.8 nM), myosin light chain kinase (Ki = 20 nM), protein kinase A (Ki = 18 nM), protein kinase C (Ki = 25 nM), protein kinase G (Ki = 20 nM), NGF receptor gp140trk (IC50 = 3 nM), its transforming trk oncogenes, and the related neurotrophin receptors gp145trkB and gp145trkC. Reported to induce apoptosis and cell cycle arrest by decreasing Cdk1 and Cdc25c activity in T98G cells and inhibit Flt3 phosphorylation in Flt3/Itd-BaF3 cells (IC50<50 nM). Also available as a premade 1 mM (100 µg/214 µl) solution in DMSO (Cat. No. 420297).

Biochem/physiol Actions

Primary Target
CaM kinase II
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

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Cools, J., et al. 2004. Cancer Res. 64, 6385.
Chin, L.S., et al. 1999. Cancer Invest. 17, 391.
Tapley, P., et al. 1992. Oncogene 7, 371.
Hashimoto, Y. 1991. Biochem. Biophys. Res. Commun. 181, 423.
Nakanishi, S. 1988. J. Biol. Chem. 263, 6215.
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

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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