A cell-permeable (R)-DRF053 (Cat. No.
219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC
50 = 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 (IC
50 = 0.9 µM) and GSK-3α/β (IC
50 ≥30 µM). Both (R)- & (S)-CR8 are much more effective than (R)-Roscovitine (Cat. Nos.
550360 &
550364) in apoptosis induction in cell cultures.
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Product information
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Form
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Off-white solid
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Molar mass
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431.5
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Protect from Light
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Yes
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Packaged under inert gas
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Yes
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Purity
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≥97% by HPLC
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Solubility
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DMSO or EtOH
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Chemical formula
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C24H29N7O
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Store and ship information
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Storage
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+2°C to +8°C
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Ship
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Ambient Temperature Only
Standard Handling
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