MCL1 Targeted Library

ChemDiv’s MCL1 Targeted Library contains 12,000 compounds.

Myeloid cell leukemia-1 (MCL-1), a member of antiapoptotic BCL-2 family proteins. MCL-1 is widely expressed in human tissues and is primarily located in the mitochondria in cells, in which it inserts into the mitochondrial membrane via a hydrophobic tail. The antiapoptotic function of MCL-1 is essential to cell survival and homeostasis. Amplification and overexpression of MCL-1 have been reported in various human tumors, including hematological malignancies and solid tumors.

Given the critical roles of BCL-2 family proteins in maintaining cellular homeostasis, perturbation of the complexes between pro- and antiapoptotic BCL-2 proteins or their levels of expression could alter the cellular homeostatic balance and lead to overcoming apoptosis. Such imbalances can lead to the immortalization of cancers. To achieve the effects of controlling cell fate, small molecules have been developed to compensate for the imbalance between pro- and antiapoptotic BCL-2 proteins and restore the apoptotic pathway. Significant progress has been made in the development of small-molecule MCL-1 inhibitors in recent years, and three MCL-1 selective inhibitors have advanced to clinical trials. [1]

[1] W. Xiang, C. Y. Yang, and L. Bai, “MCL-1 inhibition in cancer treatment,” Onco. Targets. Ther., vol. 11, pp. 7301–7314, 2018, doi: 10.2147/OTT.S146228.