A second-generation analog of (R)-roscovitine that inhibits Cdk1

(R)-CR8 – 1 mg

Brand:
Cayman
CAS:
294646-77-8
Storage:
-20
UN-No:
Non-Hazardous - /

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy.{21810} (R)-CR8 is a second-generation analog of (R)-roscovitine (Item No. 10009569) that inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk9/cyclin T with IC50 values of 0.09, 0.072, 0.041, 0.11, and 0.18 μM, respectively.{21811,21809} (R)-CR8 has 2- to 4-fold improved potency for the inhibition of CDKs over (R)-roscovitine and can inhibit the proliferation of various cancer cell lines with ~40-fold more potency than (R)-roscovitine (IC50s ~ 0.39 versus 27.8 μM, respectively).{21811,21809} (R)-CR8 also inhibits casein kinase 1 (CK1δ/ε) with an IC50 value of 0.40 μM and inhibits GSK3α/β with an IC50 value of 12 μM.{21811}  

 

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Description

A second-generation analog of (R)-roscovitine that inhibits Cdk1, 2, 5, and 9 (IC50s = 0.09, 0.072-0.041, 0.11, and 0.18 μM, respectively) with improved potency over its parent compound; also inhibits CK1δ/ε (IC50 = 0.40 μM) and GSK-3α/β (IC50 = 12 μM)

Formal name: 2R-[[9-(1-methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol

Synonyms: 

Molecular weight: 431.5

CAS: 294646-77-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|Casein Kinase Signaling

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