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11β-hydroxysteroid dehydrogenase type 2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (10) Drug Metabolite (1) Endogenous Metabolite (1) Glucocorticoid Receptor (1) Mineralocorticoid Receptor (1) OAT (1)
By Research Areas:	Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (10)

Targets Recommended:

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150701

INCB13739	Glucocorticoid Receptor Mineralocorticoid Receptor 11β-HSD	Metabolic Disease
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC₅₀ values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research .

HY-W741510

21-Deoxy cortisone 21-Desoxycortisone; NSC 38722	Endogenous Metabolite	Cardiovascular Disease
21-Deoxy Cortisone (21-Desoxycortisone; NSC 38722) is a corticosteroid metabolite of 11-ketoprogesterone. It is formed from 11-ketoprogesterone by the cytochrome P450 (CYP) isozyme CYP17A1, but can also be produced by oxidation of 21-deoxycortisone (HY-113405) by 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2). Congenital adrenal hyperplasia is an inborn error of metabolism characterized by a deficiency of 21-hydroxylase, and 21-Deoxy Cortisone levels are elevated in patients with congenital adrenal hyperplasia.

HY-148682

18β-Glycyrrhetyl-3-O-sulfate Glycyrrhetic acid 3-O-hydrogen sulfate	OAT 11β-HSD Drug Metabolite	Metabolic Disease Inflammation/Immunology
18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC₅₀ of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research .

HY-105286

BI-135585	11β-HSD	Metabolic Disease
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC₅₀ of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research .

HY-122028

HSD-016	11β-HSD	Metabolic Disease
HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC₅₀ values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research .

HY-120643A

BMS-823778	11β-HSD	Metabolic Disease
BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes .

HY-10555

AMG-221	11β-HSD	Metabolic Disease
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a K_i of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC₅₀ of 10.1 nM in cell-based assays . AMG-221 can be used for the research of type 2 diabetes .

HY-161449

JTT-654	11β-HSD	Metabolic Disease
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC₅₀ of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC₅₀ value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .

HY-107124

BMS-770767	11β-HSD	Metabolic Disease
BMS-770767 is an 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor in type 2 diabetes. 11β-HSD1 is an important enzyme that is widely expressed in liver, adipose tissue and other tissues and plays an important role in metabolic diseases such as diabetes and obesity .

HY-14156

11β-HSD1-IN-15	11β-HSD	Metabolic Disease
11β-HSD1-IN-15 is an inhibitor of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1). 11β-HSD1-IN-15 blocks the conversion of corticosterone to cortisol by binding to the active site of the 11β-HSD1 enzyme. 11β-HSD1-IN-15 can be used to investigate the role of 11β-HSD1 enzymes IN the development of metabolic syndrome, obesity, cognitive decline and type 2 diabetes .

HY-105286A

BI-135585 hydrate	11β-HSD	Metabolic Disease
BI-135585 hydrate is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC₅₀ of 13 nM. BI-135585 hydrate exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 hydrate can be used for type 2 diabetes research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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11β-hydroxysteroid dehydrogenase type 2

Inhibitors & Agonists