GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL[1].
IC 50
Mcl-1: 0.6 μM (Ki)
References
[1] Gong Q, et al. Discovery of Phenylpyrazole Derivatives as a New Class of Selective Inhibitors of MCL-1 with Antitumor Activity. ACS Omega. 2024 Jun 13;9(25):27369-27396. DOI:10.1021/acsomega.4c02021