17β-HSD

17beta-HSD; 17β-hydroxysteroid dehydrogenases; 17 beta-hydroxysteroid dehydrogenase

17β-HSD (17β-Hydroxysteroid Dehydrogenases) is a class of NADPH/NAD+ dependent oxidoreductases that primarily catalyze the reversible conversion between the 17β-hydroxyl and ketone groups of steroid hormones, playing a crucial role in the synthesis, activation, and inactivation of steroids. The 17β-HSD family mainly belongs to the short-chain dehydrogenase/reductase (SDR) family, with the exception of 17β-HSD5 (AKR1C3), which belongs to the aldo-keto reductase (AKR) family. To date, 14 different mammalian 17β-HSDs have been identified, of which 12 are expressed in human tissues, exhibiting diverse tissue distributions, subcellular localizations, and catalytic preferences (oxidation or reduction).
17β-HSD1 primarily catalyzes the conversion of estrone (E1) to estradiol (E2) and is associated with breast cancer, prostate cancer, and endometriosis. 17β-HSD2 catalyzes the oxidation of E2 to E1, while also regulating the interconversion between androstenedione (A4) and testosterone (T), playing a role in osteoporosis. 17β-HSD3 promotes the conversion of A4 to T and is crucial for male sexual differentiation. 17β-HSD4 is involved in fatty acid β-oxidation and steroid hormone inactivation. Additionally, 17β-HSD5 participates in steroid hormone and prostaglandin synthesis, whereas 17β-HSD7 is involved in cholesterol and estrogen biosynthesis. 17β-HSD10 exhibits broad substrate specificity, contributing to the metabolism of fatty acids, bile acids, and neurosteroids, and has been implicated in Alzheimer's disease (AD). The development of selective inhibitors targeting specific 17β-HSD isoforms has become an important strategy in related disease research^[1].

References:

[1]. Marchais-Oberwinkler S, et al. 17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: protein structures, functions, and recent progress in inhibitor development. J Steroid Biochem Mol Biol. 2011 May;125(1-2):66-82. [Content Brief]

17β-HSD Related Products (156):

By Effects:	Inhibitors (151) Activator (1) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-161212

HSD17B13-IN-8	Inhibitor	99.97%
HSD17B13-IN-8 (1) is a 17β-Hydroxysteroid dehydrogenases (HSD17B13) inhibitor, with IC₅₀ values of <0.1 μM for Estradiol and <1 μM for LTB3. Used in NAFLD (Nonalcoholic fatty liver diseases) research.

HY-131586

3,7-Dihydroxyflavone		98.04%
3,7-Dihydroxyflavone (Resogalangin) is a flavonoid phytoestrogen, which can be isolated from Adenophora species. 3,7-Dihydroxyflavone is a modulator of estrogen receptors and an inhibitor of human progesterone metabolizing enzyme AKR1C1 and fungal 17β-hydroxysteroid dehydrogenase and a redox inhibitor (IC₅₀=0.6 and 6.0 μM, respectively). 3,7-Dihydroxyflavone is a fluorescent binding substrate for human serum albumin (HSA) with excitation wavelengths of 370 nm (pH 7.4) and 350 nm (pH 3.5), respectively, and emission wavelength of 515 nm.

HY-156736

HSD17B13-IN-3	Inhibitor	99.78%
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor with IC₅₀s of 0.38 μM and 0.45 μM in biochemical assays using both β-estradiol or Leukotriene B4 (LTB4) as substrate and NAD⁺ as cofactor. HSD17B13-IN-3 shows low cell penetration.

HY-W024692

Indomethacin methylester	Inhibitor	99.92%
Indomethacin methylester (Compound 10; Indometacin methylester) is a potent and selective AKR1C3 inhibitor with an IC₅₀ value of 5.67 μM. Indomethacin methylester is promising for research of postate cancer.

HY-157630

HSD17B13-IN-10	Inhibitor
HSD17B13-IN-10 (Compound 464) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of 0.01 μM. HSD17B13-IN-10 can be used in the research of liver diseases.

HY-161227

HSD17B13-IN-43	Inhibitor	99.68%
HSD17B13-IN-43 is a selective inhibitor of HSD17B13 that competitively blocks the activity of this enzyme. HSD17B13-IN-43 exhibits an IC₅₀ ≤ 0.1 µM in in vitro assays. HSD17B13-IN-43 can be used in studies of non-alcoholic steatohepatitis, fatty liver disease and hepatic fibrosis.

HY-W267205

3-Acetyl-7-Hydroxycoumarin	Inhibitor
3-Acetyl-7-Hydroxycoumarin (Compound 2) is a high selective 17-beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitor. 3-Acetyl-7-Hydroxycoumarin shows a significant improvement of the inhibitory potency, with 57% inhibition of 17β-HSD1 at 6 μM. 3-Acetyl-7-Hydroxycoumarin is promising for research of hormone-dependent diseases, such as breast cancer and endometriosis.

HY-172122

FXR/HSD17B13 modulator 1	Modulator
FXR/HSD17B13 modulator 1 (compound 6) is a potent modulator of FXR/HSD17B13. FXR/HSD17B13 modulator 1 plays an important roel in metabolic dysfunction-associated steatohepatitis (MASH) research.

HY-19903R

ASP-9521 (Standard)	Inhibitor
ASP-9521 (Standard) is the analytical standard of ASP-9521. This product is intended for research and analytical applications. ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.

HY-W016604

4'-Hydroxyvalerophenone	Inhibitor	99.96%
4'-Hydroxyvalerophenone (Compound 4) is an inhibitor of 17β-hydroxysteroid dehydrogenase (17β-HSD) with an IC₅₀ of 60.52 μM.

HY-164221

Rapirosiran	Inhibitor
Rapirosiran is a N-acetylgalactosamine-conjugated small-interfering RNA targeting liver-expressed hydroxysteroid 17-beta dehydrogenase 13 (HSD17B13) mRNA. Loss-of-function variants in the HSD17B13 associated with reduced risk of chronic liver disease. Rapirosiran can be used for the study of Non-alcoholic steatohepatitis.

HY-163243

HSD17B13-IN-29	Inhibitor
HSD17B13-IN-29 (Compound 53) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of ≤ 0.1 μM for estradiol. HSD17B13-IN-29 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH, as well as drug-induced liver injury (DILI).

HY-163249

HSD17B13-IN-49	Inhibitor
HSD17B13-IN-49 (Compound 81) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of ≤ 0.1 μM for estradiol. HSD17B13-IN-49 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH, as well as drug-induced liver injury (DILI).

HY-161229

HSD17B13-IN-69	Inhibitor
HSD17B13-IN-69 (Compound 11) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of ≤ 0.1 μM for estradiol. HSD17B13-IN-69 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH, as well as drug-induced liver injury (DILI).

HY-157708

HSD17B13-IN-67	Inhibitor
HSD17B13-IN-67 (Compound 677) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of < 0.1 μM for estradiol. HSD17B13-IN-67 can be used for research on liver diseases or metabolic disorders.

HY-155535

17β-HSD10-IN-2	Inhibitor
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer.

HY-157722

HSD17B13-IN-73	Inhibitor
HSD17B13-IN-73 (Compound 85) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of < 0.1 μM for estradiol. HSD17B13-IN-73 can be used for research on liver diseases or metabolic disorders.

HY-157717

HSD17B13-IN-70	Inhibitor
HSD17B13-IN-70 (Compound 39) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of < 0.1 μM for estradiol. HSD17B13-IN-70 can be used for research on liver diseases or metabolic disorders.

HY-162223

HSD17B13-IN-97	Inhibitor
HSD17B13-IN-97 (compound 4) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor with an IC₅₀ value of ≤0.1 µM. HSD17B13-IN-97 has the potential for the research of Nonalcoholic fatty liver diseases (NAFLDs), nonalcoholic steatohepatitis (NASH) or or drug induced liver injury (DILI).

HY-164138

17β-HSD5 inhibitor 3	Inhibitor
17β-HSD5 inhibitor 3 (Compound 31) is an orally active inhibitor for 17β-HSD5 with an IC₅₀ of 69 nM.

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