bcl2in2

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-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.