Bfl-1 Inhibitor

ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC₅₀=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with K_i of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

A-1210477 is a potent and selective inhibitor of MCL-1 with a K_i of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.

Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC₅₀s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression.

Bfl-1-IN-6 TFA is an orally active BFL1 inhibitor with an IC₅₀ of 19 nM. Bfl-1-IN-6 TFA selectively binds covalently to BFL1, stabilizes the protein and displaces BIM from BFL1, thereby inducing apoptosis activity. Bfl-1-IN-6 TFA stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor activity in mouse models. Bfl-1-IN-6 TFA can be used for the research of hematological malignancies.

Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a K_d of 0.23 nM and a K_i of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, K_d>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.

MLS-0053105, a chloromaleimide, is a selective BFL-1 inhibitor with an IC₅₀ of 0.4 µM for Bfl-1/F-Bid. MLS-0053105 shows over 10 times less potent inhibition of Bcl-W, Bcl-2, and Bcl-XL and no activity against Bcl-B and Mcl-1.

Bfl-1-IN-2 (Compound 13) is a reversible and covalent inhibitor of Bfl-1 (IC₅₀: 4.3 μM). Bfl-1-IN-2 acts by binding to Cys55 of Bfl-1.

Bfl-1-IN-7 (Compound 25) is a selective, covalent, orally active Bfl-1 inhibitor with an IC₅₀ of 0.015 μM. Bfl-1-IN-7 elicits Caspase activation. Bfl-1-IN-7 can be used in cancer research.