420298-M

K-252a, Nocardiopsis sp.

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

• Synonyme(s) : K-252a, Nocardiopsis sp.
• Formule empirique (notation de Hill): C₂₇H₂₁N₃O₅
• Numéro CAS: 97161-97-2
• Poids moléculaire : 467.47
• Code UNSPSC : 12352202
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 1 mg/mL; DMF: soluble
• 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, 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).

Actions biochimiques/physiologiques

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

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable