CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer.
CYP19A1/CYP11B2-IN-1 (Compound X21) (0.001-100 μM, 24 h) shows a time- and concentration-dependent proliferation inhibition on MCF-7 and MDA-MB-231 cells[1].CYP19A1/CYP11B2-IN-1 (700 nM, 24 h) significantly inhibits the phosphorylation of mTOR in MCF-7 cells, thereby negatively modulating the PI3K/Akt/mTOR axis[1].CYP19A1/CYP11B2-IN-1 (20-30 μM) has no significant inhibition of hERG and Nav1.5, indicating no toxicity to the heart[1].
References:
[1]. Tinivella A, et al. Discovery of a Potent Dual Inhibitor of Aromatase and Aldosterone Synthase. ACS Pharmacology & Translational Science. 2023 Nov 23.