17β-hsd 13

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].

HSD17B13-IN-10 (Compound 464) serves as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of 0.01 μM. It is useful in liver disease research [1].

HSD17B13-IN-100 (compound 34), an inhibitor of HSD17B13, exhibits an IC50 of less than 0.1 μM with estradiol [1].

HSD17B13-IN-100 (compound 37) acts as an inhibitor for HSD17B13, demonstrating an inhibitory concentration (IC 50) of less than 0.1 μM with Estradiol [1].

HSD17B13-IN-11 (Compound 2), with IC50 values of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol, effectively inhibits hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). This compound is utilized in studying various medical conditions including liver diseases, metabolic and cardiovascular disorders, particularly non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI) [1].

HSD17B13-IN-12 (Compound 3), functioning as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC 50 value of ≤ 0.1 μM against both leukotriene B3 and estradiol. This compound is applicable in studying various conditions including liver diseases, metabolic disorders, and cardiovascular diseases like NAFLD or NASH, as well as drug-induced liver injury (DILI) [1].

HSD17B13-IN-13 (Compound 5), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrates potent activity with an IC 50 value of less than 0.1 μM against estradiol. This compound is applicable in the study of liver diseases, including NAFLD [1].

HSD17B13-IN-14 (Compound 4) acts as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), achieving an IC 50 of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol. This compound is utilized in studying various conditions, including liver diseases, metabolic disorders, and cardiovascular diseases like NAFLD or NASH, as well as drug-induced liver injury (DILI) [1].

HSD17B13-IN-15 (Compound 6) acts as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting IC 50 values of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol. This compound finds applications in studying various conditions, including liver diseases, metabolic disorders, and cardiovascular diseases such as NAFLD, NASH, or drug-induced liver injury (DILI) [1].

HSD17B13-IN-16 (compound 8) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC50 of <0.1 μM and <1 μM when using estradiol and Leukotriene B3 as substrates, respectively. The compound is notably significant in the treatment of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-17 (compound 9) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). It demonstrates inhibitory efficacy with IC50 values of ＜0.1 μM for estradiol and ＜1 μM for Leukotriene B3 as substrates. This compound is significant in the management of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-18 (compound 13) serves as a potent inhibitor of hydroxysteroid 17?-dehydrogenase 13 (HSD17B13), exhibiting IC50 values of ＜ 0.1 μM for estradiol and ＜ 1 μM for Leukotriene B3 as substrates. This compound is crucial in managing nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-19 (compound 16) acts as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting IC50 values under 0.1 μM and under 1 μM when using estradiol and Leukotriene B3 as substrates, respectively. This compound is crucial in the treatment of nonalcoholic fatty liver diseases (NAFLDs), such as nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-21 (compound 17) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 of < 0.1 μM for estradiol and < 1 μM for Leukotriene B3 as substrates. This compound plays a crucial role in the management of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].