Chemical Structure : CIRc-004
CAS No.:
3036232-05-7
CIRc-004
(CIRc004)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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994.90
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Formula
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C45H59Cl2F6N7O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,4R)-N-((S)-3-cyclobutyl-1-(((6S,9S,12S)-6-(2,5-dichlorobenzyl)-9-isobutyl-7-methyl-5,8,11,18-tetraoxo-4,7,10,17-tetraazaspiro[2.15]octadecan-12-yl)(methyl)amino)-1-oxopropan-2-yl)-1-(3,3-difluoro-1-(trifluoromethyl)cyclobutane-1-carbonyl)-4-fluoropyrrolidine-2-carboxamide
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References
1. Singh S, et al. Nature. 2025 Aug 20. doi: 10.1038/s41586-025-09433-w.
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