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.

• Synonym(s): Cdk2/9 Inhibitor, (4-(2-Amino-4-methylthiazol-5-yl)pyrimidin-2-yl)-(3-nitrophenyl)amine, Cdk7 Inhibitor III
• Empirical Formula (Hill Notation): C₁₄H₁₂N₆O₂S
• CAS Number: 507487-89-0
• Molecular Weight: 328.35
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: 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)
• InChI key: DYTKVFHLKPDNRW-UHFFFAOYSA-N

Description

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable