(R)-CR8
Modify Date: 2024-01-10 18:36:54
(R)-CR8 structure
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Common Name | (R)-CR8 | ||
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| CAS Number | 1786438-30-9 | Molecular Weight | 540.92 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C24H32Cl3N7O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of (R)-CR8(R)-CR8 trihydrochloride (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[1][2]. |
| Name | (R)-CR8 trihydrochloride |
|---|
| Description | (R)-CR8 trihydrochloride (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[1][2]. |
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| Related Catalog | |
| Target |
CDK1/cyclinB1:0.09 μM (IC50) cdk2/cyclin A:0.072 μM (IC50) CDK2/cyclinE:0.041 μM (IC50) Cdk5/p25:0.11 μM (IC50) CDK7/cyclin H:1.1 μM (IC50) CDK9/Cyclin T:0.18 μM (IC50) CK1δ/ε:0.4 μM (IC50) |
| In Vitro | (R)-CR8 trihydrochloride (CR8 trihydrochloride) (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[1]. (R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage[1]. Apoptosis Analysis[1] 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. |
| In Vivo | (R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment[2]. Animal Model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g)[2] Dosage: 5 mg/Kg Administration: i.p. Result: Resulted in a significant reduction in lesion size. |
| References |
| Molecular Formula | C24H32Cl3N7O |
|---|---|
| Molecular Weight | 540.92 |