495621

Olomoucine II

A cell-permeable 2,6,9-trisubstituted purine analog that acts as a potent, reversible, and ATP-competitive inhibitor of Cdk1/B.

• Synonym(s): Olomoucine II, 6-(2-Hydroxybenzylamino)-2-((1R)-(hydroxymethyl)propyl)amino)-9-isopropylpurine
• Empirical Formula (Hill Notation): C₁₉H₂₆N₆O₂
• CAS Number: 500735-47-7
• Molecular Weight: 370.45
• MDL number: MFCD06411574
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: colorless
• solubility: DMSO: 1 mg/mL; ethanol: 1 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C19H26N6O2/c1-4-14(10-26)22-19-23-17(20-9-13-7-5-6-8-15(13)27)16-18(24-19)25(11-21-16)12(2)3/h5-8,11-12,14,26-27H,4,9-10H2,1-3H3,(H2,20,22,23,24)
• InChI key: NDUVSANREQEDRE-UHFFFAOYSA-N

Description

General description

A cell-permeable 2,6,9-trisubstituted purine analog that acts as a potent, reversible, and ATP-competitive inhibitor of Cdk1/B with an IC₅₀ of 20 nM and displays increased potency over purvalanol A (Cat. No. 540500; IC₅₀ = 50 nM), Roscovitine (Cat. No. 557360; IC₅₀ = 450 nM), Bohemine (Cat. No. 203600; IC₅₀ = 1.1 µM) and Olomoucine (Cat. No. 495620; IC₅₀ = 7.0 µM). Further, exerts greater in vitro cytotoxicity in various cancer cell lines (IC₅₀ = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM and 11.1 µM for CEM, MCF7, HOS, G631 and K562, respectively).

A cell-permeable, potent, reversible, and ATP-competitive inhibitor of Cdk1/cyclin B (IC₅₀ = 20 nM) that displays increased potency over purvalanol A (Cat. No. 540500; IC₅₀ = 50 nM), Roscovitine (Cat. No. 557360; IC₅₀ = 450 nM), Bohemine (Cat. No. 203600; IC₅₀ = 1.1 µM), and Olomoucine (Cat. No. 495620; IC₅₀ = 7.0 µM). Also exhibits greater in vitro cytotoxicity in various cancer cell lines (IC₅₀ = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM, and 11.1 µM for CEM, MCF7, HOS, G631, and K562, respectively).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Cdk1/B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 20 nM against Cdk1/B

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

Krystof, V., et al. 2002. Bioorg. Med. Chem. Lett.12, 3283.

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