420297

K-252a, Nocardiopsis sp.

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

• Sinonimo/i: InSolution K-252a, Nocardiopsis sp.
• Formula empirica (notazione di Hill): C₂₇H₂₁N₃O₅
• Numero CAS: 97161-97-2
• Peso molecolare: 467.47
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Stato: liquid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: −20°C
• Stringa SMILE: [n]21c3c4[n](c6c(c4c7c(c3c8c2cccc8)CNC7=O)cccc6)C5OC1(C(C5)(O)C(=O)OC)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); KOZFSFOOLUUIGY-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Stato fisico

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

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 10 - Combustible liquids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Punto d’infiammabilità (°C): 87 °C - closed cup - (Dimethylsulfoxide)