(R)-CR8

SKU: orb1220030

Description

(R)-CR8 is a potent and selective CDK inhibitor.A delayed systemic post-LFP administration at 3 hours of CR8--a potent second-generation cyclin-dependent kinase (CDK) inhibitor--reduced CCA; cortical, hippocampal, and thalamic neuronal loss; and cortical microglial and astrocyte activation. Furthermore, CR8 treatment attenuated sensorimotor and cognitive deficits, alleviated depressive-like symptoms, and decreased lesion volume.

Key Properties

• CAS Number: 294646-77-8
• MW: 431.53
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₉N₇O
• SMILES: CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c2ccccn2)c2ncn(C(C)C)c2n1
• Target: CDK
• Solubility: In Vitro: DMSO : 50 mg/mL (115.87 mM)

Bioactivity

• In Vivo:
  (R)-CR8 (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment. Animal model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g). Dosage: i.p. Administration: 5 mg/Kg. Result: Resulted in a significant reduction in lesion size.
• In Vitro:
  (R)-CR8 (CR8) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC50 of 0.49 μM for SH-SY5Y cell line. (R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage. The CDK-bound form of (R)-CR8 has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation. 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

Alternative Names

CR8 ,(R)-Isomer

Quick Database Links

Gene Symbol

CDK