Venetoclax (ABT-199, GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with Ki value of <0.01 nM.
Venetoclax (ABT-199) displays >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1.
Venetoclax (ABT-199) potently induces apoptosis in FL5.12-BCL-2 cells (EC50=261 nM) and reduces tumor burden in chronic lymphocytic leukemia (CLL) primary samples (EC50 =3 nM).
Venetoclax (ABT-199 enhances efficacy of clinically relevant chemotherapy and immunotherapy drugs.
Venetoclax (ABT-199) exhibits binding to SARS-CoV-2 3C-like protease (3CLpro) active site in a virtual screen.
Venetoclax (ABT-199) reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.
