Bcl 2 IN 2

Bcl-2-IN-2 is a highly potent and selective inhibitor targeting Bcl-2 and Bcl-xL, displaying an IC50 value of 0.034 nM against Bcl-2 and 43 nM against Bcl-xL, demonstrating over 1000-fold selectivity for Bcl-2 compared to Bcl-xL.

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

Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.

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-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-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.

Bcl-2-IN-21 (compound C1), an iridium-based anticancer agent, effectively targets and inhibits Bcl-2, thereby impeding cancer cell colony formation and promoting increased levels of Bax and caspase 3.

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.

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-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.

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

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.

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.

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

Bcl-2/Mcl-1-IN-5 (Compound S6) is an inhibitor targeting Bcl-2 and Mcl-1. It facilitates apoptosis by downregulating anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane depolarization, and activates caspase-dependent apoptotic cascades, as evidenced by Caspase-3 activation and PARP1 cleavage. Additionally, Bcl-2/Mcl-1-IN-5 exhibits anti-hepatocellular carcinoma activity.

Bcl-2/Mcl-1-IN-1 is an inhibitor of Bcl-2 (Ki: 4.53 μM) and Mcl-1 (Ki: 1.19 μM), and can be used in cancer research.

Bcl-2/Mcl-1-IN-2 is an inhibitor of Bcl-2 [Ki: 4.70 μM] and Mcl-1 [Ki: 0.88 μM], suitable for use in cancer research.

Bcl-2/Mcl-1-IN-3 is a Bcl-2/Mcl-1 inhibitor, targeting Mcl-1 (Ki: 0.14 μM) and Bcl-2 (Ki: 0.23 μM), suitable for cancer research.

Bcl-2-IN-7 is a potent inhibitor of Bcl-2 (b-cell lymphoma-2), which can downregulate the expression of Bcl-2, increase the expression of p53, Bax, caspase-7 mRNA, and induce cell cycle arrest and apoptosis in MCF-7 cells of breast cancer. Bcl2-IN-7 showed good antitumor activity against MCF-7 cells (IC50: 20.17 μM), LoVo cells (IC50: 22.64 μM), HepG2 cells (IC50: 45.57 μM) and A549 cells (IC50: 51.50 μM).

Bcl-2-IN-6 is a potent inhibitor of Bcl-2 (b-cell lymphoma-2) that downregulates Bcl-2 expression and increases the expression of p53, Bax, and caspase-7 mRNA. bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. bcl-2-IN-7 acts on MCF-7 cells ( Bcl2-IN-7 showed good antitumor effects on MCF-7 cells (IC50: 20.91 μM), LoVo cells (IC50: 22.30 μM), HepG2 cells (IC50: 42.29 μM) and A549 cells (IC50: 48.00 μM).

Bcl-2-IN-9 is a novel, pro-apoptotic, low cytotoxic Bcl-2 inhibitor (IC50: 2.9 μM) that downregulates Bcl-2 expression, induces apoptosis in cancer cells, and exhibits high selectivity for leukemia cells.

Bcl-2-IN-8 is a potent anti-cancer agent that exhibits anti-proliferative effects on both drug-sensitive and drug-resistant cancer cells, inhibits cell migration in a dose-dependent manner, blocks the cell cycle in the G1 phase, and induces apoptosis. Bcl-2-IN-8 has shown research potential in [triple-negative breast cancer].