420297

K-252a, Nocardiopsis sp.

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

• Sinônimo(s): InSolution K-252a, Nocardiopsis sp.
• Fórmula empírica (Notação de Hill): C₂₇H₂₁N₃O₅
• Número CAS: 97161-97-2
• Peso molecular: 467.47
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: liquid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• Condições de expedição: wet ice
• temperatura de armazenamento: −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)
• chave InChI: KOZFSFOOLUUIGY-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

forma física

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

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 10 - Combustible liquids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Ponto de fulgor (°C): 87 °C - closed cup - (Dimethylsulfoxide)