(R)-CR8 trihydrochloride

Research use only, not for human use.

(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) is a CDK1/2/5/7/9 inhibitor that acts as a molecular glue degrader with neuroprotective activity and induces apoptosis.

(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.

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.

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.

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Apoptosis

Apoptosis

Apoptosis | CDK

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1786438-30-9

540.92

C24H32Cl3N7O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (92.44 mM; Ultrasonic )

Cl.Cl.Cl.CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c2ccccn2)c2ncn(C(C)C)c2n1

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(-20℃)

With Ice Pack

≥ 2 years