BCL

ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.

TL4-12 is a specific MAP4K2/GCK inhibitor that inhibits IKZF1 and BCL-6.TL4-12 inhibits MM cell proliferation and induces apoptosis, and can be used in the study of multiple myeloma (MM).

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin's lymphoma.

Bcl-B inhibitor 1 is an antitumor compound that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

BCL6-IN-3 is a potent BCL6 inhibitor with GI50 of 70 nM in SU-DHL4 cells. BCL6-in-3 regulates cell activation, differentiation, DNA damage and apoptosis, and has antitumor activity.

MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 4.45 μM and 3.18 μM, respectively [1].

MCL-1/BCL-2-IN-2 is a potent and selective dual inhibitor of Bcl-2 and Mcl-1.

MCL-1/BCL-2-IN-3 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 5.95 and 4.78 μM, respectively.

MCL-1/BCL-2-IN-4 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2.

BCL6-IN-8c is an orally active and potent inhibitor of B-cell lymphoma 6 (BCL6)-corepressor interaction(IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay).

Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.

BCL-XL-IN-3 (Compound 11) is an inhibitor of BCL-XL, with a Ki of less than 0.01 nM. It suppresses cell viability in both normal Molt-4 cells and digitonin-permeabilized Molt-4 cells, with EC50 values of 77.8 nM and 0.07 nM, respectively. BCL-XL-IN-3 can be utilized as an ADC toxin for synthesizing Clezutoclax.

Bcl-2-IN-18 (Compound 23) is a Bcl-2 inhibitor targeting breast cancer with an IC50 value of 4.7 μM against MCF-7 cells. It exhibits antitumor activity.

Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor used specifically to target breast cancer.

Bcl-2-IN-20 (Compound 81) is a Bcl-2 inhibitor with an IC50 of less than 10 μM, achieving a 79.1% inhibition rate at 9 μM. It demonstrates cytotoxicity in cell lines such as SK-MEL-28 (IC50 > 10 μM), A549 (IC50 = 6.1 μM), HepG2 (IC50 > 10 μM), MCF-7 (IC50 = 8.9 μM), HCT116 (IC50 > 10 μM), and HEK-293 (IC50 = 14.1 μM). Bcl-2-IN-20 also promotes the generation of ROS, inducing apoptosis and DNA damage.

BCL-xLligand 2 is a ligand for BCL-xL. It can be conjugated with an E3 ligase ligand and a linker to form the Bcl-xL-targeting PROTAC degrader PZ671.

GPER/Bcl-2 Inhibitor is a GPER/Bcl-2 inhibitor that suppresses the proliferation of glioblastoma cells and the formation of neurospheres. It is applicable in glioblastoma (GBM) research.

Bcl-2-IN-23 (compound 5) is a selective inhibitor targeting Bcl-2. It demonstrates an IC50 range of 25.7-33.7 μM in HTB-140, HeLa, and SW620 cells. Acting through non-covalent competitive binding to the Bcl-2 protein, Bcl-2-IN-23 significantly reduces Bcl-2 expression, inducing late-stage apoptosis and necroptosis in cancer cells. By disrupting the Bcl-2-mediated mitochondrial apoptotic inhibition pathway, it increases cancer cell susceptibility to apoptosis and reduces the release of the inflammatory factor IL-6. Bcl-2-IN-23 is applicable in anti-apoptosis research for malignant tumors such as melanoma, cervical cancer, and colorectal cancer.

BCL-XL-IN-4 (compound 10) is a potent and selective BCL-XL inhibitor, exhibiting Ki values of 0.042 nM for BCL-XL and 170 nM for BCL-2. Additionally, BCL-XL-IN-4 demonstrates cytotoxic properties.

PROTACBcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader with significant antitumor activity against HepG2 and HUVEC cells. It induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTACBcl-xL degrader-4 markedly inhibits tumor growth in xenograft mouse models.

Bcl-2-IN-24 (Compound 11g) is a potent and selective Bcl-2 inhibitor with a Kd value of 11.3 μM. It exhibits antiproliferative activity against HCT-116 and A549 cells, effectively inhibiting tumor cell colony formation and inducing apoptosis. Bcl-2-IN-24 is applicable in the study of colon cancer and lung cancer.

PROTACBCL-xL/BCL-w Degrader 1 (Compound 44) is a PROTAC degrader that targets BCL-xL and BCL-w. It demonstrates significant anticancer activity while minimizing toxicity to platelets.

BCL6-IN-4, a potent inhibitor of B-cell lymphoma 6 (BCL6), exhibits anti-tumor activities with an inhibitory concentration 50 (IC50) value of 97 nM[1].