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 (155):

By Effects:	Inhibitors (150) Activator (1) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-107379

AKR1C3-IN-1	Inhibitor	98.21%
AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC₅₀ of 13 nM.

HY-148814

BI-3231	Inhibitor	99.83%
BI 3231, a chemical probe, is a potent and selective hydroxysteroid 17β-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-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-152189

S19-1035	Inhibitor	99.93%
S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC₅₀ value of 3.04 nM. S19-1035 can be used for the research of tumor.

HY-164221B

Rapirosiran sodium scrambled negative control	Inhibitor
Rapirosiran sodium scrambled negative control is the sequence scrambled negative control of Rapirosiran sodium.

HY-183280

17β-HSD10/CDK5-IN-1	Inhibitor
17β-HSD10/CDK5-IN-1 is a poent dual 17β-HSD10 and CDK5 inhibitor with IC₅₀s of 2.44 and 0.26 μM for 17β-HSD10 and CDK5, respectively. 17β-HSD10/CDK5-IN-1 reduces ROS accumulation, attenuates pathological Tau phosphorylation, reduces Aβ plaque deposition, and ameliorates cognitive deficits in Alzheimer's mice. 17β-HSD10/CDK5-IN-1 can be used for the research of Alzheimer's disease.

HY-182028

17β-HSD10-IN-4	Inhibitor
17β-HSD10-IN-4 is a selective brain-penetrant 17β-HSD10 inhibitor with an IC₅₀ of 6.33 μM. 17β-HSD10-IN-4 forms key interactions with the 17β-HSD10 catalytic triad to functionally inhibit the enzyme, without altering its protein levels. 17β-HSD10-IN-4 restores mitochondrial function, reduces ROS levels, increases ATP production, and suppresses cytochrome c release. 17β-HSD10-IN-4 attenuates CDK5/p25 activation, reduces Tau hyperphosphorylation, Aβ plaque load and restores brain-derived neurotrophic factor levels. 17β-HSD10-IN-4 improves cognitive function.17β-HSD10-IN-4 can be used for the research of Alzheimer's disease.

HY-145433

17β-HSD1-IN-1	Inhibitor	99.79%
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-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	98.51%
6-Bromocoumarin (compound 34) is a potential anti-bacterial agent, with no inhibition against 17β-HSD1. 6-Bromocoumarin exhibtis affinity for α and β estrogen receptors.

HY-155534

17β-HSD10-IN-1	Inhibitor
17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability. 17β-HSD10-IN-1 doesn't result additional effects for mitochondrial off-targets and cytotoxic or neurotoxic effects.

HY-159525

Linustedastatum	Inhibitor	98.10%
Linustedastatum (Linustedastat; FOR-6219) is an orally active hydroxysteroid 17-beta dehydrogenase 1 (HSD17B1) inhibitor. Linustedastatum can be used for the study of endometriosis.

HY-103394

TC HSD 21	Inhibitor	99.0%
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-164221A

Rapirosiran sodium	Inhibitor
Rapirosiran sodium 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 sodium can be used for the study of Non-alcoholic steatohepatitis.

HY-149040

Odafosfamide	Inhibitor	99.06%
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research.

HY-129583

Lepidiline A	Activator	99.54%
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-156735

HSD17B13-IN-2	Inhibitor	99.72%
HSD17B13-IN-2 is an HSD17B13 inhibitor with human IC₅₀ values of 0.18 μM (with β-estradiol as substrate) and 0.25 μM (with Leukotriene B4 as substrate), and it exhibits selectivity for human HSD17B11. HSD17B13-IN-2 binds to the active site of HSD17B13 in an NAD⁺-dependent manner, interacts with the bound NAD⁺ cofactor, and stabilizes human HSD17B13 protein to prevent its aggregation. HSD17B13-IN-2 reduces the conversion of β-estradiol to estrone in cellular assays. HSD17B13-IN-2 can be used in studies related to nonalcoholic fatty liver disease.

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-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.

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