Bcl-W Inhibitor

Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a K_i of less than 0.01 nM. Venetoclax induces autophagy.

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-x_L, Bcl-2 and Bcl-w, with a K_i of less than 1 nM.

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.

A-1331852 is an orally available BCL-XL selective inhibitor with a K_i of less than 10 pM.

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.

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

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.

Navitoclax (Standard) (ABT-263 (Standard)) is the analytical standard of Navitoclax (HY-10087). This product is intended for research and analytical applications. Navitoclax (ABT-263 ) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a K_i value of <1 nM for each target. Navitoclax triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax alleviates fibrosis and induces thrombocytopenia. Navitoclax exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases.

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.

Navitoclax-d₈ is the d₈-labeled Navitoclax (HY-10087). Navitoclax (ABT-263 ) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a K_i value of <1 nM for each target. Navitoclax triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax alleviates fibrosis and induces thrombocytopenia. Navitoclax exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases.

Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.

Navitoclax dihydrochloride (ABT-263 dihydrochloride) is an orally active BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with a K_i value of <1 nM for each target. Navitoclax dihydrochloride triggers endogenous Apoptosis and downregulates the expression of Survivin and TGFβ2. Navitoclax dihydrochloride alleviates fibrosis and induces thrombocytopenia. Navitoclax dihydrochloride exhibits anticancer activity against a variety of tumors and enhances the efficacy of chemotherapy and radiotherapy. Navitoclax dihydrochloride can be used in the research of acute lymphoblastic leukemia, ovarian cancer, and fibrotic diseases.