Mcl-1 inhibitor 6 is a potent, orally active small molecule that selectively targets the anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1). Mcl-1 inhibitor 6 binds with high affinity, with a dissociation constant (K d) of 0.23 nM, and exhibits binding activity with a K i of 0.02 μM. Mcl-1 inhibitor 6 displays exceptional selectivity over other anti-apoptotic Bcl-2 family proteins, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, all of which display binding constants greater than 10 μM. Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity in preclinical models, highlighting its potential as a therapeutic candidate in oncology.

BCL-XL:>10 μM (Kd), BCL2A1:>10 μM (Kd), BCL-W:>10 μM (Kd), Bcl-2:10 μM (Ki), Bfl-1:1.57 μM (Ki), Bcl-2:>10 μM (Kd), MCL1:0.02 μM (Ki), MCL1:0.23 nM (Kd)