420297

K-252a, Nocardiopsis sp.

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

• Synonyme(s) : InSolution K-252a, Nocardiopsis sp.
• Formule empirique (notation de Hill): C₂₇H₂₁N₃O₅
• Numéro CAS: 97161-97-2
• Poids moléculaire : 467.47
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Conditions d'expédition: wet ice
• Température de stockage: −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)
• Clé InChI: KOZFSFOOLUUIGY-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Forme physique

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.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 10 - Combustible liquids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Point d'éclair (°C): 87 °C - closed cup - (Dimethylsulfoxide)