238806

Cdk2/9 Inhibitor

The Cdk2/9 Inhibitor, also referenced under CAS 507487-89-0, controls the biological activity of Cdk2/9. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Cdk2/9 Inhibitor, (4-(2-Amino-4-methylthiazol-5-yl)pyrimidin-2-yl)-(3-nitrophenyl)amine, Cdk7 Inhibitor III
• Formule empirique (notation de Hill): C₁₄H₁₂N₆O₂S
• Numéro CAS: 507487-89-0
• Poids moléculaire : 328.35
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 25 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C14H12N6O2S/c1-8-12(23-13(15)17-8)11-5-6-16-14(19-11)18-9-3-2-4-10(7-9)20(21)22/h2-7H,1H3,(H2,15,17)(H,16,18,19)
• Clé InChI: DYTKVFHLKPDNRW-UHFFFAOYSA-N

Description

Description générale

A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (K_i = 2 nM and 4 nM, respectively). It also inhibits GSK-3β, Cdk4/D₁, Cdk7/H, Cdk1/B, and Abl at higher concentrations (K_i = 20, 53, 70, 80, and 160 nM, respectively), but exhibits little activity towards 9 other kinases (K_i >1.0 µM). Shown to inhibit phosphorylation of cellular Cdk substrates, pRb and RNA polymerase II, and Cdk2-mediated S-phase transition.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Cdk2/E and Cdk9/T1

Product competes with ATP.

Reversible: no

Target K_i: 2 nM and 4 nM against Cdk2/E and Cdk9/T1, respectively

Conditionnement

Packaged under inert gas

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

Kontopidis, G., et al. 2006. Chem. Biol.13, 201.
Wang, S., et al. 2004. J. Med. Chem.47, 1662.

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