Cyclin A/B RxL-IN-2

SKU: orb3211105

Description

Cyclin A/B RxL-IN-2 is a macrocyclic peptide Cyclin A/B inhibitor with oral bioavailability. It exhibits an IC50 of 0.05 μM and a Kd of 2.7 nM for Cyclin A, and an IC50 of less than 0.02 μM and a Kd of 1.0 nM for Cyclin B. This compound competitively binds to the hydrophobic pocket (HP) of Cyclin A/B, blocking their interaction with substrate RxL motifs, inducing replication stress, DNA damage, mitosis, and apoptosis in E2F overexpressing cells. In NCI-H69 and NCI-H446 small cell lung cancer xenograft models, Cyclin A/B RxL-IN-2 demonstrates tumor growth inhibition and regression, making it useful for related small cell lung cancer research.

Key Properties

• CAS Number: 3064485-73-7
• MW: 962.46
• Formula: C₄₅H₆₂ClF₆N₇O₇
• SMILES: C(=O)(C1(C(F)(F)F)CC(F)(F)C1)N2[C@H](C(N[C@H](C(N(C)[C@@H]3C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC4=C(OC5CC5)N=CC(Cl)=C4)C(=O)N(C)CCCCCCC3)=O)[C@@H]6CC6)=O)C[C@@H](F)C2
• Target: CDK,Apoptosis

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CDK,Apoptosis