17β-HSD Inhibitor

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

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

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

2,2-Bis(p-hydroxyphenyl)-1,1,1-trichloroethane-d₈ is the deuterated-labeled HPTE (HY-W490804). HPTE is the active in vivo metabolite of Methoxychlor (HY-B1873), and acts as an inhibitor of 3β‑HSD and 17β‑HSD3. HPTE binds to the substrate-binding pocket of 3β‑HSD in a non-competitive manner, but competitively occupies the coenzyme NAD⁺-binding site, thereby inhibiting the conversion of pregnenolone to progesterone. HPTE binds to the androstenedione-binding pocket (the substrate pocket) of 17β‑HSD3 in a non-competitive manner, and competitively occupies the coenzyme NADPH-binding site, thus blocking the conversion of androstenedione to testosterone. HPTE interferes with androgen biosynthesis in Leydig cells by inhibiting the activities of these two key steroidogenic enzymes. HPTE can be used in studies related to androgen biosynthesis.

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).

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).

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).

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.

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.

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.

S34-1040 is an AKR1C3 inhibitor with a human IC₅₀ of 0.03 μM and exhibits no detectable inhibition of AKR1C1, AKR1C2, or AKR1C4. S34-1040 functions as a chemosensitizer and restores sensitivity of doxorubicin-resistant breast cancer cells to doxorubicin. S34-1040 can be used for the research of doxorubicin-resistant breast cancer.

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.

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).

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

HSD17B13-IN-15 (Compound 6) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol. HSD17B13-IN-15 can be used in the research of liver diseases, metabolic disorders, or cardiovascular diseases such as NAFLD or NASH, or drug-induced liver injury (DILI).

HSD17B13-IN-93 (Compound 9) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value for estradiol that is greater than 0.1 μM and less than or equal to 0.5 μM. HSD17B13-IN-93 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).

HSD17B13-IN-6(Compound 475) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of 0.01 μM. HSD17B13-IN-6can be used in the research of liver diseases.

HSD17B13-IN-80-d₂ (Compound 200) is the the deuterium labeled HSD17B13-IN-80 (HY-163263). HSD17B13-IN-80 is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC₅₀ value of ≤ 0.1 μM for estradiol. HSD17B13-IN-80 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).

17β-HSD10-IN-3 (compound 23) is a 17β-HSD10 inhibitor with the IC₅₀ of 5.59 μM. 17β-HSD10-IN-3 shows no cell cytotoxicity toward the HEK-293 cell line up to 20 μM.

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.