219494
Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem
The Cdk/CKI Inhibitor, (R)-DRF053, also referenced under CAS 1186647-87-9, controls the biological activity of Cdk/CKI. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem, 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate
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About This Item
Empirical Formula (Hill Notation):
C23H27N7O · xH2O
CAS Number:
Molecular Weight:
417.51 (anhydrous basis)
UNSPSC Code:
12352200
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
ethanol: 30 mg/mL, DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1,CDK5, and CK1 activity (IC50 = 220,80,14 vs. 350, 200, 2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih 100 µM respective compound).
A cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1/CDK5/CK1 activity (IC50 = 220/80/14 vs. 350/200/2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih100 µM respective compound).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Oumata, N., et al. J. Med. Chem.51, 5229.
Bettayeb, K., et al. 2008. Oncogene27, 5797.
Bettayeb, K., et al. 2008. Oncogene27, 5797.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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