OLOMOUCINE II

Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 μM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity[1].

ChEBI: 2-[[[2-(1-hydroxybutan-2-ylamino)-9-propan-2-yl-6-purinyl]amino]methyl]phenol is a thiopurine.

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).

Cell permeable: yes

CDK9/cycT: 0.06 μM (IC₅₀); CDK2/cyclinE: 0.1 μM (IC₅₀); CDK7/cyclin H: 0.45 μM (IC₅₀); Cdk1/cyclin B: 7.6 μM (IC₅₀); CDK4/cyclinD1: 19.8 μM (IC₅₀)

[1] Krystof V, et al. Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor. Cell Mol Life Sci. 2005 Aug;62(15):1763-71. DOI:10.1007/s00018-005-5185-1