2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. 11β-HSD

11β-HSD

11beta-HSD; 11β-hydroxysteroid dehydrogenases; 11 beta-hydroxysteroid dehydrogenase

Two isozymes of 11β-hydroxysteroid dehydrogenase (11β-HSD) catalyze interconversion of active cortisol and corticosterone with inert cortisone and 11-dehydrocorticosterone. 11β-HSD type 1 (11β-HSD1), a predominant reductase in most intact cells, catalyzes the regeneration of active glucocorticoids, thus amplifying cellular action. 11β-HSD1 is selectively elevated in adipose tissue in obesity where it contributes to metabolic complications. Similarly, 11β-HSD1 is elevated in the ageing brain where it exacerbates glucocorticoid-associated cognitive decline. Deficiency or selective inhibition of 11β-HSD1 improves multiple metabolic syndrome parameters in rodent models and human clinical trials and similarly improves cognitive function with ageing. 11β-HSD2 is a high-affinity dehydrogenase that inactivates glucocorticoids. In the distal nephron, 11β-HSD2 ensures that only aldosterone is an agonist at mineralocorticoid receptors (MR). 11β-HSD2 inhibition or genetic deficiency causes apparent mineralocorticoid excess and hypertension due to inappropriate glucocorticoid activation of renal MR. The placenta and fetus also highly express 11β-HSD2 which, by inactivating glucocorticoids, prevents premature maturation of fetal tissues and consequent developmental “programming.”

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107124
    BMS-770767
    		Inhibitor 99.90%
    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.
    BMS-770767
  • HY-123800
    BI 187004
    		98.13%
    BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research.
    BI 187004
  • HY-101930
    BMS-816336
    		Inhibitor 99.86%
    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.
    BMS-816336
  • HY-101930A
    (Rac)-BMS-816336
    		Inhibitor 99.91%
    (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.
    (Rac)-BMS-816336
  • HY-148454
    Necroptosis-IN-3
    		Inhibitor 99.77%
    Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis. Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1.
    Necroptosis-IN-3
  • HY-14393R
    Emodin (Standard)
    		Inhibitor
    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.
    Emodin (Standard)
  • HY-122028
    HSD-016
    		Inhibitor 99.95%
    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.
    HSD-016
  • HY-W129359
    11β-HSD1-IN-8
    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.
    11β-HSD1-IN-8
  • HY-U00325
    11β-HSD1-IN-1
    		Inhibitor 99.80%
    11β-HSD1-IN-1 is an inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1), with an IC50 of 52 nM, and used for the treatment of pain.
    11β-HSD1-IN-1
  • HY-114464S
    11-Beta-hydroxyandrostenedione-d4
    		Inhibitor 98.3%
    11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor.
    11-Beta-hydroxyandrostenedione-d<sub>4</sub>
  • HY-14393S
    Emodin-d4
    		Inhibitor
    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-d<sub>4</sub>
  • HY-148682R
    18β-Glycyrrhetyl-3-O-sulfate (Standard)
    		Inhibitor
    (Z)-Methyl icos-11-enoate (Standard) is the analytical standard of (Z)-Methyl icos-11-enoate. This product is intended for research and analytical applications. (Z)-Methyl icos-11-enoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    18β-Glycyrrhetyl-3-O-sulfate (Standard)
  • HY-118113
    BVT-116429
    		Inhibitor
    BVT-116429 is an 11βHSD1 inhibitor with the activity of increasing adiponectin concentration and improving glucose homeostasis in diabetic mice. BVT-116429 can increase plasma adiponectin levels in diabetic KKAy mice, reduce basal insulin levels, and reduce fasting blood glucose levels after 10 days of inhibition, similar to the effect of rosiglitazone.
    BVT-116429
  • HY-10555
    AMG-221
    		Inhibitor
    AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki 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.
    AMG-221
  • HY-W324243
    11β-HSD1-IN-9
    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.
    11β-HSD1-IN-9
  • HY-123090
    11β-HSD1-IN-12
    		Inhibitor
    11β-HSD1-IN-12 is a 11β-HSD1 inhibitor (Example 21 in reference patent). 11β-HSD1 regenerates active glucocorticoids from inactive forms and is important in regulating intracellular glucocorticoid concentration. 11β-HSD1-IN-12 can be used in the research of obesity and metabolic syndrome.
    11β-HSD1-IN-12
  • HY-151627
    11β-HSD1-IN-11
    		Inhibitor
    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.
    11β-HSD1-IN-11
  • HY-W324220
    11β-HSD1-IN-10
    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.
    11β-HSD1-IN-10
  • HY-120643A
    BMS-823778
    		Inhibitor
    BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes.
    BMS-823778
  • HY-W342082
    11-Ketoprogesterone
    		Substrate 98.44%
    11-Ketoprogesterone (11KP4) is the substrate for CYP17A1 and 11β-HSD2 that could be metabolized to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF) with glucocorticoid activity.
    11-Ketoprogesterone
Cat. No. Product Name / Synonyms Application Reactivity