238803

Cdk2 Inhibitor III

The Cdk2 Inhibitor III, also referenced under CAS 199986-75-9, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Cdk2 Inhibitor III, 2( bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine, CVT-313, 2(bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine, CVT-313
• Empirical Formula (Hill Notation): C₂₀H₂₈N₆O₃
• CAS Number: 199986-75-9
• Molecular Weight: 400.47
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C20H28N6O3/c1-14(2)26-13-22-17-18(21-12-15-4-6-16(29-3)7-5-15)23-20(24-19(17)26)25(8-10-27)9-11-28/h4-7,13-14,27-28H,8-12H2,1-3H3,(H,21,23,24)
• InChI key: NQVIIUBWMBHLOZ-UHFFFAOYSA-N

Description

General description

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ = ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Cdk2/A, Cdk2/E

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Bhattacharjee, R.N., et al. 2001. Mol. Cell. Biol.21, 5417.
Brooks, E.E., et al. 1997. J. Biol. Chem.272, 29207.

Legal Information

Sold under license of U.S. Patents 6,617,331 and 6,803,371.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1