bfl-1

Bfl-1-IN-6 is a high-affinity Bfl-1/A1 inhibitor (IC50 = 19 nM). It neutralizes anti-apoptotic effects by binding to the hydrophobic groove of Bfl-1, sensitizing cancer cells to chemotherapy in hematological malignancy research.

Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor of Bfl-1, demonstrating an IC50 of 0.022 μM. This compound enhances the activity of caspase-3/7, with an EC50 of 0.37 μM, and also inhibits the viability of SU-DHL-1 cells, showing an EC50 of 1.3 μM.

Bfl-1-IN-1 (Compound 15) is a potent and selective inhibitor of Bfl-1. It inhibits Bfl-1 with a Ki of 0.63 μM and Mcl-1 with a Ki of 6.77 μM.

Bfl-1-IN-4 (Compound 8) is an inhibitor of the Bcl-2-related protein A1 (Bfl-1) with an IC50 of 16.8 μM.

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

Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM).

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.

UMI-77 is a selective Mcl-1 inhibitor. UMI-77 binds to the BH3-binding groove of Mcl-1 with a Ki of 490 nM and is selective over other members of the Bcl-2 family.

Sabutoclax (BI-97C1)(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

MLS-0053105, a chloromaleimide, functions as a selective inhibitor of BFL-1, exhibiting an IC50 of 0.4 µM against Bfl-1/F-Bid. Its inhibitory potency is over tenfold lower for Bcl-W, Bcl-2, and Bcl-XL, and it shows no activity against Bcl-B and Mcl-1.

S65487 (VOB560) is a potent and selective inhibitor of the anti-apoptotic protein Bcl-2, displaying activity not only against the wild-type protein but also against clinically relevant BCL-2 mutations such as G101V and D103Y. S65487 demonstrates poor affinity toward other Bcl-2 family members, including MCL-1, BFL-1, and BCL-XL, which underlines its selectivity profile. S65487 induces apoptosis in cancer cells and exhibits robust anticancer activities in preclinical studies.

S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is effective against BCL-2 mutations, including G101V and D103Y, while exhibiting poor affinity for MCL-1, BFL-1, and BCL-XL. This compound induces apoptosis and possesses anticancer activities.

S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, demonstrates activity against BCL-2 mutations, including G101V and D103Y, while showing poor affinity for MCL-1, BFL-1, and BCL-XL. It induces apoptosis and possesses anticancer activities.

A-1293201 is a potent and selective Bfl-1/A1 inhibitor (IC50 = 16 nM). It neutralizes anti-apoptotic signaling by binding the hydrophobic groove, used for hematological malignancy resistance research.

(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].

Gambogic Acid (Standard) is a reference standard for research and analysis in studies involving Gambogic Acid. Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.