CR8, (S)-Isomer - CAS 1084893-56-0 - Calbiochem

A cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC₅₀ = 0.15, 0.080, 0.060, 0.12, 0.11, and 0.61 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK9/T, and CK1δ/ε, respectively). Although (S)-CR8 displays in general similar kinase inhibitory profile as its (R)-enantiomer (Cat. No. 203881 ), it does exhibit more enhanced and reduced activity against, respectively, Dyrk1A (IC₅₀ = 0.9 µM) and GSK-3α/β (IC₅₀ ≥ 30 µM). Both (R)- and (S)-CR8 are much more effective than (R)-Roscovitine (Cat. Nos. 550360 and 550364 ) in apoptosis induction in cell cultures.

A cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC₅₀ = 0.15, 0.080, 0.060, 0.12, 0.11, and 0.61 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK9/T, and CK1δ/ε, respectively). Although (S)-CR8 displays in general similar kinase inhibitory profile as its (R)-enantiomer (Cat. No. 203881), it does exhibit more enhanced and reduced activity against, respectively, Dyrk1A (IC₅₀ = 0.9 µM) and GSK-3α/β (IC₅₀ ≥30 µM). Both (R)- & (S)-CR8 are much more effective than (R)-Roscovitine (Cat. Nos. 550360 & 550364) in apoptosis induction in cell cultures.

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

Bettayeb, K., et al. 2008. Oncogene27, 5797.

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Toxicity: Standard Handling (A)