CR8, (S)-Isomer A cell-permeable (R)-DRF053 analog

CR8, (S)-Isomer (CAS 1084893-56-0)

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Synonym: (2S)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol
Application: A cell-permeable (R)-DRF053 analog
CAS Number: 1084893-56-0
Purity: ≥97%
Molecular Weight: 431.5
Molecular Formula: C24H29N7O
* Refer to Certificate of Analysis for lot specific data (including water content).
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CR8, (S)-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 Cdc2(CDK1)/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35 (p25), CDK7/cyclin H, CDK9/cyclin T, and casein kinase I δ/ε (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, ERK 2, and GSK-3α/β, respectively). Both (R)-CR8 and (S)-enantiomers are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.


References

1. Bettayeb, K., et al., 2008. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 27(44): 5797-807. PMID: 18574471

Physical State :
Solid
Solubility :
Soluble in DMSO (35 mg/ml), and ethanol (20 mg/ml).
Storage :
Store at -20° C
Refractive Index :
n20D 1.66 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
25211051
SMILES :
CC[C@@H](CO)NC1=NC2=C(C(=N1)NCC3=CC=C(C=C3)C4=CC=CC=N4)N=CN2C(C)C

Download SDS (MSDS)

Certificate of Analysis

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