C3249

CR8

≥95% (HPLC)

• Synonym(s): (2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1, (R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine, C&R8
• Empirical Formula (Hill Notation): C₂₄H₂₉N₇O
• CAS Number: 294646-77-8
• Molecular Weight: 431.53
• MDL number: MFCD18785641
• UNSPSC Code: 12352200
• PubChem Substance ID: 329775030
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: powder
• color: off-white
• solubility: DMSO: ≥10 mg/mL
• storage temp.: 2-8°C
• SMILES string: CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c3ccccn3)c4ncn(C(C)C)c4n1
• InChI: 1S/C24H29N7O/c1-4-19(14-32)28-24-29-22(21-23(30-24)31(15-27-21)16(2)3)26-13-17-8-10-18(11-9-17)20-7-5-6-12-25-20/h5-12,15-16,19,32H,4,13-14H2,1-3H3,(H2,26,28,29,30)/t19-/m1/s1
• InChI key: HOCBJBNQIQQQGT-LJQANCHMSA-N

Description

Biochem/physiol Actions

CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation.

CR8 is a potent inhibitor of CDK1/2/5/7/9.

Features and Benefits

This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable