Cyclin A/B RxL-IN-2 is a macrocyclic peptide that acts as a selective inhibitor of Cyclin A and Cyclin B. It exhibits high potency with an IC50 of 0.05 μM for Cyclin A and less than 0.02 μM for Cyclin B, alongside Kd values of 2.7 nM and 1.0 nM, respectively. This compound competes for binding at the hydrophobic patch of Cyclin A/B, disrupting interactions with the substrate RxL motif, leading to replication stress and DNA damage in E2F-high cells, as well as inducing mitotic catastrophe and apoptosis. Cyclin A/B RxL-IN-2 demonstrates efficacy in inhibiting tumor growth in NCI-H69 and NCI-H446 small cell lung cancer xenograft models, making it a valuable tool for research in small-cell lung cancer.
Cyclin A/B RxL-IN-2 is a macrocyclic peptide that acts as a selective inhibitor of Cyclin A and Cyclin B. It exhibits high potency with an IC50 of 0.05 μM for Cyclin A and less than 0.02 μM for Cyclin B, alongside Kd values of 2.7 nM and 1.0 nM, respectively. This compound competes for binding at the hydrophobic patch of Cyclin A/B, disrupting interactions with the substrate RxL motif, leading to replication stress and DNA damage in E2F-high cells, as well as inducing mitotic catastrophe and apoptosis. Cyclin A/B RxL-IN-2 demonstrates efficacy in inhibiting tumor growth in NCI-H69 and NCI-H446 small cell lung cancer xenograft models, making it a valuable tool for research in small-cell lung cancer.
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