420298-M

K-252a, Nocardiopsis sp.

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

• Synonym(s): K-252a, Nocardiopsis sp.
• Empirical Formula (Hill Notation): C₂₇H₂₁N₃O₅
• CAS Number: 97161-97-2
• Molecular Weight: 467.47
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

General description

A cell-permeable, reversible, and ATP-competitive inhibitor against multiple protein kinases, including, but not limited to, CaM kinase II (K_i = 1.8 nM), myosin light chain kinase (K_i = 20 nM), protein kinase A (K_i = 18 nM), protein kinase C (K_i = 25 nM), protein kinase G (K_i = 20 nM), NGF receptor gp140^trk (IC₅₀ = 3 nM), its transforming trk oncogenes, and the related neurotrophin receptors gp145^trkB and gp145^trkC. 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 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

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable