Chemical Structure : CIRc-004
货号: PC-25358Not For Human Use, Lab Use Only.
CIRc-004 is a potent, cell-permeable dual cyclin A/B RxL inhibitor with IC50 of 0.13 and <0.02 uM for cyclin A1-CDK2 and cyclin B-CDK1, does not inhibit cyclin E1-CDK2, inhibits cyclin A/B-RxL interactions and induces apoptosis in cancer cells with high E2F activity.
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CIRc-004 is a potent, cell-permeable dual cyclin A/B RxL inhibitor with IC50 of 0.13 and <0.02 uM for cyclin A1-CDK2 and cyclin B-CDK1, does not inhibit cyclin E1-CDK2, inhibits cyclin A/B-RxL interactions and induces apoptosis in cancer cells with high E2F activity.
Non-transformed WI-38 fibroblasts is insensitive to cyclin A/B inhibition.
CIRc-004 induces apoptosis and mitotic arrest in sensitive SCLC (NCI-H1048, H446 and H69).
CIRc-004 blocks anaphase initiation, consistent with SAC activation causing mitotic cell death.
CIRc-004 disrupts an interaction between cyclin B and an RxL-containing substrate that normally functions as a negative regulator of cyclin B–CDK1 activity.
CIRc-004 induces E2F1 hyperactivation and sensitizes cells to cyclin A/B RxL inhibitors.
分子量 | 994.90 | |
分子式 | C45H59Cl2F6N7O7 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Singh S, et al. Nature. 2025 Aug 20. doi: 10.1038/s41586-025-09433-w.
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