CR8, (R)-Isomer A cell-permeable, ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor

CR8, (R)-Isomer (CAS 294646-77-8)

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Solicitud: A cell-permeable, ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor
Número de CAS: 294646-77-8
Pureza: ≥97%
Peso Molecular: 431.5
Fórmula Molecular: C24H29N7O
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CR8, (R)-Isomer is a cell-permeable (R)-DRF053 (sc-221408) 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 (cyclin dependent kinase 1/B), CDK2/A (cyclin dependent kinase 2/A), CDK2/E (cyclin dependent kinase 2/E), CDK5/p25 (cyclin dependent kinase 5/p25), CDK7/H (cyclin dependent kinase 7/H), CDK9/T (cyclin dependent kinase 9/T), and CK1δ/ε, respectively). (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/&beta (glycogen synthase kinase-3α/β), respectively). Both (R)-CR8 and (S)-enantiomers are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.


References

1. Oumata, N., et al. J. Med. Chem. 51: 5229-5242. PMID: 1869875
2. Bettayeb, K., et al. 2008. Oncogene 27: 5797-5807. PMID: 18574471

Estado de Materia :
Solid
Forma Derivada :
Synthetic
Solubilidad :
Soluble in DMSO (50 mg/ml), and ethanol (15 mg/ml).
ALMACENAMIENTO :
Store at -20° C
IC50 :
CDK1/B: IC50 = 0.09 µM; CDK2/A: IC50 = 0.07 µM; CDK2/E: IC50 = 0.04 µM; CDK5/p25: IC50 = 0.11 µM; CDK7/H: IC50 = 1.10 µM; CDK9/T: IC50 = 0.18 µM; CK1δ/ε: IC50 = 0.40 µM
Valores de pK :
pKb: 4.59 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
10224714
Número MDL :
MFCD18785641
SMILES :
CC[C@H](CO)NC1=NC2=C(C(=N1)NCC3=CC=C(C=C3)C4=CC=CC=N4)N=CN2C(C)C

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