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 (128):

By Effects:	Inhibitors (124) Activator (1) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-148814

BI-3231	Inhibitor	99.83%
BI 3231 is a potent and selective hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor, with IC₅₀s of 1 and 13 nM for hHSD17B13 and mHSD17B13, respectively. BI 3231 has the potential for the research of nonalcoholic steatohepatitis (NASH) and other liver diseases.

HY-19903

ASP-9521	Inhibitor	≥98.0%
ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC₅₀ of 11 nM for human AKR1C3.

HY-138557

AKR1C3-IN-4	Inhibitor	99.77%
AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research.

HY-107379

AKR1C3-IN-1	Inhibitor	98.23%
AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC₅₀ of 13 nM.

HY-155035

S07-1066	Inhibitor	99.48%
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells.

HY-W005186

6-Bromocoumarin	Inhibitor
6-Bromocoumarin (compound 34) is a potential 17β-HSD1 inhibitor with affinity for α and β estrogen receptors.

HY-131586

3,7-Dihydroxyflavone
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-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-145433

17β-HSD1-IN-1	Inhibitor	99.34%
17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC₅₀s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC).

HY-156735

HSD17B13-IN-2	Inhibitor	99.72%
HSD17B13-IN-2 (compound 1) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-2 has cell experimental activity.

HY-129583

Lepidiline A	Activator	99.87%
Lepidiline A exhibits cytotoxic activity against HL-60 cells with an IC₅₀ value of 32.3 μM. Lepidiline A targets HSD17B1 activity, increases the bioconversion efficiency of sex hormones (including the conversion of estrogen into 17β-estradiol and 4-androsten-3,7-dione into testosterone), thereby improving the reproductive capacity of fruit flies..

HY-156736

HSD17B13-IN-3	Inhibitor	99.78%
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-3 does not have cell experimental activity.

HY-103394

TC HSD 21	Inhibitor	99.14%
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC₅₀ of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.

HY-161227

HSD17B13-IN-43	Inhibitor	99.68%
HSD17B13-IN-43 (11) is a 17β-Hydroxysteroid dehydrogenases (HSD17B13) inhibitor, with an IC₅₀ of <0.1 μM for Estradiol. Used in NAFLD (Nonalcoholic fatty liver diseases) research.

HY-157627

HSD17B13-IN-9	Inhibitor	99.92%
HSD17B13-IN-9 (252) is a 17β-Hydroxysteroid dehydrogenases (HSD17B13) inhibitor, with an IC₅₀ of 0.01 μM for 50 nM HSD17B13. Used in NAFLD (Nonalcoholic fatty liver diseases) research.

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-128145

HSD17B13-IN-41	Inhibitor
HSD17B13-IN-41 (Compound C) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). HSD17B13-IN-41 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH.

HY-159525

Linustedastatum	Inhibitor
Linustedastatum (Linustedastat) is a hydroxysteroid 17-beta dehydrogenase 1 (HSD17B1) inhibitor.

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).

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