17β-HSD Inhibitor

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.

Obafistat is a potent aldo-keto reductase AKR1C3 inhibitor with an IC₅₀ of 1.2 nM for human AKR1C3 (patent WO2017202817A1, example 4).

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).

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.

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.

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

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.

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.

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

TC HSD 21 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) against related 17β-HSD isozymes, with an IC₅₀ of 14 nM in HeLa cells. TC HSD 21 can be used in the research of prostate cancer.

Rapirosiran (ALN-HSD) sodium is a HSD17β13-targeting siRNA. Rapirosiran sodium can be used for the research of metabolic dysfunction-associated steatohepatitis.

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.

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.

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.

HSD17B13-IN-1 (compound 2) is a ppotent inhibitor of hydroxysteroid 17?-dehydrogenase 13 (HSD17B13), with the IC₅₀ of ＜ 0.1 μM? estradiol? as substrates. HSD17B13-IN-1? plays an important role in nonalcoholic fatty liver diseases (NAFLDs) including NASH (nonalcoholic steatohepatitis).

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.

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.

Gatuzosiran, a siRNA,is a 17-beta-hydroxysteroid dehydrogenase 13 (HSD17B13) synthesis reducer. It is used for the study of fatty liver disease.

SN34037 is a specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188) with the ability to inhibit the cytotoxic activity of PR-104A. SN34037-sensitive coumberone reduction provides a rapid and specific assay for AKR1C3 activity. SN34037 inhibits the aerobic cytotoxicity of PR-104A in TF1 erythroleukemia cells with high AKR1C3 expression, but not in Nalm6 pre-B acute lymphoblastic leukemia cells with low AKR1C3 expression.

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.