17β-hsd10

17β-HSD10-IN-1 is an orally available 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) inhibitor with blood-brain permeability and potency for the study of Alzheimer's disease.

17β-HSD10-IN-3 (compound 23) serves as an inhibitor of 17β-HSD10, exhibiting an IC50 value of 5.59 μM. Importantly, this compound demonstrates no cytotoxic effects on the HEK-293 cell line at concentrations up to 20 μM [1].

17β-HSD10-IN-2 (compound 11), a benzothiazolylurea-based inhibitor, specifically targets 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10), avoiding mitochondrial off-targets and cytotoxic or neurotoxic effects. This multifunctional mitochondrial enzyme inhibitor has potential applications in Alzheimer's disease (AD) and hormone-dependent cancer research [1].

ESC1002755 is an inhibitor of 17β-HSD10 with an IC50 of 19 nM. Notably enzyme-specific, ESC1002755 exhibits non-competitive inhibition against the cofactor NADH. At a concentration of 50 μM, it shows minimal cytotoxicity in HEK293 cells. It holds potential for research in Alzheimer's disease and hormone-dependent cancers such as prostate, bone, and colorectal cancers.