203881
CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem
Synonym(s):
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
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General description
A cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 μM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos. 550360 & 550364), while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 μM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both (R)-CR8 & its (S)-enantiomer (Cat. No. 203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
A cell-permeable (R)-DRF053 analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 μM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine, while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 μM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both the (R)-CR8 and (S)-enantiomer are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
A cell-permeable (R)-DRF053 analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Storage Class
11 - Combustible Solids
wgk
WGK 3
Regulatory Information
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Nassima Oumata et al.
Journal of medicinal chemistry, 51(17), 5229-5242 (2008-08-14)
Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key molecular features of Alzheimer's disease, production of amyloid-beta peptides (extracellular plaques) and hyper-phosphorylation of Tau (intracellular neurofibrillary tangles). A series of 2,6,9-trisubstituted purines, structurally related to
K Bettayeb et al.
Oncogene, 27(44), 5797-5807 (2008-06-25)
Among the ten pharmacological inhibitors of cyclin-dependent kinases (CDKs) currently in clinical trials, the purine roscovitine (CYC202, Seliciclib) is undergoing phase 2 trials against non-small-cell lung and nasopharyngeal cancers. An extensive medicinal chemistry study, designed to generate more potent analogues