(R)-CR8 trihydrochloride

SKU: orb2901732

Description

(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.

Key Properties

• CAS Number: 1786438-30-9
• MW: 540.92
• Purity: >98% (HPLC)
• Formula: C₂₄H₃₂Cl₃N₇O
• SMILES: Cl.Cl.Cl.CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c2ccccn2)c2ncn(C(C)C)c2n1
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 50 mg/mL (92.44 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g). Dosage: 5 mg/Kg. Administration: i.p. Result: Resulted in a significant reduction in lesion size.
• In Vitro:
  Apoptosis Analysis Cell line: SH-SY5Y cell line. Concentration: 0.1, 1, 10, 100 μM Incubation time: 24 hours. Result: Reduced cell survival in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Apoptosis