17β-hsd

17β-HSD7-IN-1 (compound 4) acts as an inhibitor of 17β-HSD7, effectively suppressing the formation of estradiol with an IC50 value of 63 nM.

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-HSD5 inhibitor 1 (Compound 29) is a potent inhibitor of 17β-HSD5, exhibiting an IC50 value of 2.9 nM in HEK-293 cells that overexpress human 17β-HSD5.

17β-HSD5 inhibitor 2 (Compound 30) is an inhibitor of 17β-hydroxysteroid dehydrogenase 5 (17β-HSD5), with an IC50 of 40 nM.

17β-HSD1-IN-1 (Compound 1) is a highly selective inhibitor of 17β-HSD1 with IC50 values of 5.6 nM for 17β-HSD1 and 3155 nM for 17β-HSD2, and it can be used in non-small cell lung cancer (NSCLC) research [1].

Steroid sulfatase/17β-HSD1-IN-1 is a highly effective inhibitor of steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities, with an IC50 value of 28 nM against cellular human steroid sulfatase. This compound holds significant potential for investigating estrogen-dependent diseases [1].

Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a potent dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity (IC50= 63 nM) and has research value in endometriosis and other estrogen-dependent diseases.

Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 [17β-HSD1], useful in studying endometriosis and other estrogen-dependent diseases.

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].

Steroid sulfatase/17β-HSD1-IN-5 is an irreversible inhibitor of steroid sulfatase (STS) and a reversible, selective inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), with IC50 values of 43 nM for 17β-HSD1 and 6.2 μM for 17β-HSD2. This compound is utilized in research related to metabolic diseases, particularly endometriosis [1].

17β-HSD5 inhibitor 3 (Compound 31) is an orally effective inhibitor of 17β-HSD5, exhibiting an IC50 of 69 nM.

11β-HSD1 inibitor 17 is an inhibitor of 11β-hydroxysteroid dehydrogenase (11β-HSD1).

PTOTAC HSD17B13 Degrader 1, a PROTAC designed to target 17β-HSD 13 (HSD17B13), incorporates several key components. These include the PROTAC target protein ligand HSD17B13 Degrader 2, the PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate, and the E3 ubiquitin ligase ligand E3 Ligase Ligand 31. Notably, the conjugate formed by the E3 ubiquitin ligase ligand and the linker is recognized as E3 Ligase Ligand-linker Conjugate 114.

HSD17B13 degrader 2, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is designed for synthesis applications.

FXR/HSD17B13 modulator 1 (compound 6) is an effective modulator of FXR/HSD17B13, playing a significant role in studies related to metabolic dysfunction-associated steatohepatitis (MASH).

HSD17B13-IN-4 (Compound 95) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with a Ki value for the substrate estradiol LCMS of ≤ 50 nM. It can be utilized in research on liver diseases, metabolic disorders, or cardiovascular diseases such as NAFLD, NASH, or drug-induced liver injury (DILI).

HSD17B13-IN-5 (Compound 96) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with a Ki value of ≤ 50 nM for the estradiol substrate LCMS. It is applicable in research on liver diseases, metabolic disorders, or cardiovascular conditions, such as NAFLD or NASH, or drug-induced liver injury (DILI).

HSD17B13-IN-101 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase (HSD17B13), exhibiting an IC50 value of less than 0.1 μM for estradiol. It is applicable in research on non-alcoholic fatty liver disease (WO2023146897A1; compound 94).

HSD17B13-IN-105 (Compound EX.87) is a selective inhibitor of 17β-hydroxysteroid dehydrogenase 13 (17BHSD13) with an IC50 value of 0.036 μM, demonstrating high selectivity over 17BHSD4, which has an IC50 value of 31.5 μM. HSD17B13-IN-105 shows potential for research in liver diseases such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).

HSD17B13-IN-104 (Compound 32) is an orally active and potent inhibitor of HSD17B13 with high selectivity (IC50=2.5 nM). It modulates liver lipid metabolism by inhibiting the SREBP-1c/FAS pathway and blocks the enzymatic activity of HSD17B13 to alleviate hepatic lipid accumulation. HSD17B13-IN-104 shows potential for research in metabolic dysfunction-associated fatty liver disease.

HSD17B13-IN-2 (compound 1) is a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13), exhibiting demonstrable activity in cellular experiments [1].

HSD17B13-IN-3 (compound 2) is a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13), but lacks cellular experimental activity [1].

HSD17B13-IN-1 (compound 2) acts as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC50 value of <0.1 μM with estradiol as a substrate. It plays a crucial role in addressing nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].