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human 11β-HSD-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (26) Autophagy (3) Casein Kinase (3) Endogenous Metabolite (1) Isotope-Labeled Compounds (1) Reference Standards (1) SARS-CoV (3)
By Research Areas:	Cancer (4) Inflammation/Immunology (4) Metabolic Disease (20) Neurological Disease (5)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14393

Emodin 35+ Cited Publications Frangula emodin	SARS-CoV Casein Kinase Autophagy 11β-HSD	Cancer
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective *11β-HSD1* inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

HY-124529

Lunularin	11β-HSD Endogenous Metabolite	Metabolic Disease Inflammation/Immunology Cancer
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC₅₀ of 45.44 μM and a K_i of 35.8 μM against human *11β-HSD1, and an IC₅₀* of 17.39 μM and a K_i of 10.31 μM against rat *11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB* pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human *11β-HSD1* and the steroid/NADPH-binding region of rat *11β-HSD1, but does not inhibit 11β-HSD2* or mouse *11β-HSD1*. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .

HY-18054

BVT 2733 4 Publications Verification	11β-HSD	Inflammation/Immunology
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC₅₀=96 nM) over the human enzyme (IC₅₀=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease .

HY-18056

PF-915275	11β-HSD	Metabolic Disease
PF-915275 is a potent, selective and orally active **human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a K_i of 2.3 nM and an EC₅₀** of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC₅₀ of 20 and 100 nM, respectively .

HY-18173

AZD8329	11β-HSD	Metabolic Disease
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3 .

HY-14393R

Emodin (Standard) 35+ Cited Publications Frangula emodin (Standard)	Reference Standards SARS-CoV Casein Kinase Autophagy 11β-HSD	Cancer
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective *11β-HSD1* inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

HY-151627

11β-HSD1-IN-11	11β-HSD	Neurological Disease Metabolic Disease
11β-HSD1-IN-11 (Compound c1a) is a competitive *11β-HSD1* inhibitor with IC₅₀s of 0.34 μM and 0.13 μM against rat and human 11β-HSD1, respectively .

HY-111262

ABT-384	11β-HSD	Neurological Disease Metabolic Disease
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (K_i 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .

HY-W106057

11β-HSD1-IN-7	11β-HSD	Neurological Disease Metabolic Disease
11β-HSD1-IN-7 (compound c10a) is a *11β HSD1* inhibitor with an IC₅₀ value of 1.9 μM for human 11β HSD1. 11β-HSD1-IN-7 can be used for the research of diabetes and cognitive decline .

HY-101930A

(Rac)-BMS-816336	11β-HSD	Metabolic Disease
(Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of *human* and *mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme* with IC₅₀s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability .

HY-W129359

11β-HSD1-IN-8	11β-HSD	Neurological Disease Metabolic Disease
11β-HSD1-IN-8 (compound c6a) is a *11β HSD1* inhibitor with an IC₅₀ value of 2.3 μM for human 11β HSD1. 11β-HSD1-IN-8 can be used for the research of diabetes and cognitive decline .

HY-120496

Clofutriben ASP3662	11β-HSD	Neurological Disease Metabolic Disease
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with K_i values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .

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-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-101930

BMS-816336	11β-HSD	Metabolic Disease
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC₅₀ of 3.0 nM .

HY-14393S

Emodin-d4 Frangula emodin-d₄	Isotope-Labeled Compounds SARS-CoV Casein Kinase Autophagy 11β-HSD	Cancer
Emodin-d₄ is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

HY-117428

INU-101	11β-HSD	Metabolic Disease
INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .

HY-W324243

11β-HSD1-IN-9	11β-HSD	Metabolic Disease
11β-HSD1-IN-9 (compound c4a) is a potent *11β-HSD1* inhibitor with IC₅₀ values of 0.48 and 1.3 µM for human and murine *11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1*-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment .

HY-120643

BMS-823778 hydrochloride	11β-HSD	Metabolic Disease
BMS-823778 hydrochloride is a potent, selective and orally active *11β-HSD1* inhibitor with an IC₅₀ of 2.3 nM against human 11β-HSD1 .

HY-18054A

BVT-2733 hydrochloride	11β-HSD	Inflammation/Immunology
BVT-2733 hydrochloride is a potent, selective and orally active nonsteroidal *11β-HSD1* inhibitor. BVT-2733 hydrochloride is more potent against mouse *11β-HSD1* enzyme (IC₅₀=96 nM) than against human *11β-HSD1* enzyme (IC₅₀=3341 nM). BVT-2733 hydrochloride has the potential to be used in the study of arthritis and obesity-related diseases .

HY-W324220

11β-HSD1-IN-10	11β-HSD	Metabolic Disease
11β-HSD1-IN-10 (compound c3a) is a potent *11β-HSD1* inhibitor (IC₅₀=1.8 µM for human). 11β-HSD1-IN-10 can be used in studies of obesity, hyperglycemia and cognitive impairment .

HY-162026

11β-HSD1-IN-14	11β-HSD	Metabolic Disease
11β-HSD1-IN-14 (Compound 17) is a selective inhibitor for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1), with IC₅₀ of 74 nM for human HSD1, and 603 nM for HSD1 expressed HEK293 cell .

HY-101930B

(R)-BMS-816336	11β-HSD	Metabolic Disease
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of *human, mouse* and *cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme* with IC₅₀s of 14.5 nM, 50.3 nM and 16 nM, respectively .

HY-18054R

BVT 2733 (Standard)	11β-HSD	Inflammation/Immunology
BVT 2733 (Standard) is the analytical standard of BVT 2733. This product is intended for research and analytical applications. BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease .

HY-125421

11β-HSD1-IN-26	11β-HSD	Metabolic Disease
11β-HSD1-IN-26 (Compound 9f) is a type 1 11β-hydroxysteroid dehydrogenase (11β-HSD-1) inhibitor, with an IC₅₀ of 1.6 nM against the human form and 241 nM against the murine form. 11β-HSD1-IN-26 exhibits inhibitory activity against CYP1C19, with an IC₅₀ of 2 μM. 11β-HSD1-IN-26 can be used for research on metabolic syndrome .

HY-18056R

PF-915275 (Standard)	11β-HSD	Metabolic Disease
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-14393

Emodin 35+ Cited Publications Frangula emodin	Classification of Application Fields Polygonaceae Plants Endogenous metabolite Quinones Human Gut Microbiota Metabolites Microorganisms Rheum palmatum L. Anthraquinones Phenols Polyphenols Disease Research Fields Source Classification Cancer	SARS-CoV Casein Kinase Autophagy 11β-HSD
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective *11β-HSD1* inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

HY-124529

Lunularin	Structural Classification Human Gut Microbiota Metabolites other families Conocephalum conicum (L.) Dumort. Phenols Polyphenols Plants Endogenous metabolite Source Classification	11β-HSD Endogenous Metabolite
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC₅₀ of 45.44 μM and a K_i of 35.8 μM against human *11β-HSD1, and an IC₅₀* of 17.39 μM and a K_i of 10.31 μM against rat *11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB* pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human *11β-HSD1* and the steroid/NADPH-binding region of rat *11β-HSD1, but does not inhibit 11β-HSD2* or mouse *11β-HSD1*. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .

HY-14393R

Emodin (Standard) 35+ Cited Publications Frangula emodin (Standard)	Quinones Rheum palmatum L. Classification of Application Fields Polygonaceae Phenols Plants Disease Research Fields Source Classification Cancer	Reference Standards SARS-CoV Casein Kinase Autophagy 11β-HSD
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective *11β-HSD1* inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P72237

	HSD11B1 Protein, Human (His-SUMO) 11 beta HSD 1; 11 beta HSD1 ; 11 beta hydroxysteroid dehydrogenase 1; 11 DH ; 11-beta hydroxysteroid dehydrogenase; type 1; 11-beta-HSD1; 11-DH; 11DH ; Corticosteroid 11 beta dehydrogenase isozyme 1; Corticosteroid 11-beta-dehydrogenase isozyme 1; CORTRD2; DHI1_human; HDL; HSD 11; HSD11; HSD11B; HSD11B1; HSD11L; member 1	Human	E. coli
	The proteins encoded by ED genes are involved in a variety of physiological processes. HSD11B1 Protein, Human (His-SUMO) is the recombinant human-derived HSD11B1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.

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Cat. No.	Product Name	Chemical Structure

HY-14393S

Emodin-d4
Emodin-d₄ is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

Emodin-d4

Emodin-d₄ is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .

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