Dihydrotestosterone(DHT)

Catalog No.S4757 Synonyms: androstanolone, stanolone, 5α-DHT

Dihydrotestosterone(DHT) Chemical Structure

Molecular Weight(MW): 290.44

Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.

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Biological Activity

Description Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
Targets
Androgen Receptor [1]
()
In vitro

In AR-positive bladder cancer UMUC3 and TCC-SUP cells, dihydrotestosterone (DHT) increased the expression of EGFR and ERBB2 both in mRNA and in protein levels. DHT additionally upregulated the levels of phosphorylation of EGFR (pEGFR) and its downstream proteins AKT (pAKT) and ERK1/2 (pERK), induced by EGF treatment, in AR-positive cells[1].

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / Cyclin D2 / Cyclin D3 / Cyclin E2 / Cyclin A1 / AR; 

PubMed: 26372468     


HPr-1AR cells were treated with 10 nM DHT or vehicle control for 24–48 hours (h), and immunoblot analysis of cell lysates reveals that cyclin D1 and D2 protein expression decreased substantially with DHT treatment compared to vehicle.

p-CDK2 / CDK2 / CDK4 / CDK6 / CDKN1A / p-RB / RB ; 

PubMed: 26372468     


HPr-1AR cells were treated with 10 nM DHT or vehicle control for 24–48 hours (h). Immunoblot analysis of cell lysates reveals that CDK4 and CDK6 protein expression decreased and CDKN1A expression increased with DHT treatment compared to vehicle. CDK2 phosphorylation at threonine 160 (T160) decreased nearly 50% with androgen treatment at 24 and 48 hours, albeit not significantly, and total CDK2 protein expression remained unchanged. Relative to total RB expression, the levels of various phosphorylated forms of RB (S780 and S807/811) decreased over time with androgen treatment. 

p27 / p-p27 ; 

PubMed: 22139837     


CWR22Rv1 or CWR22R3 cells were stimulated with 10 nm DHT for 6 h, with the addition of MG132 during the last 2 h before harvesting. Proteins were then immunoblotted.

AR / PP1 ; 

PubMed: 26636645     


HeLa cells were transfected with Flag-PP1α and HA-AR and then incubated for overnight in androgen-depleted medium without or with androgen (10 nM of DHT) as indicated for blotting. 

26372468 22139837 26636645
Immunofluorescence
FOXO1 / p27 ; 

PubMed: 22139837     


CWR22R3 cells cultured in medium with CDS serum were treated without/with DHT (10 nm) for 4 h. The cells were immunostained for FOXO1 and p27 and examined with a confocal microscope. 

AKT(S473) / PKCα(S657) ; 

PubMed: 22139837     


CWR22R3 cells cultured in medium with CDS serum were treated without/with 10 nm DHT (−/+ DHT) for 4 h. The cells were immunostained for AKT or PKCα phosphorylation and examined with a confocal microscope. Bars: 20 μm

22139837
In vivo DHT-treated SOD1-G93A mice demonstrate ameliorated muscle atrophy and increased body weight, which is associated with stronger grip-strength. DHT treatment increases the expression of insulin-like growth factor-1 in muscle, which can exert myotrophic as well as neurotrophic effects through retrograde transport. DHT treatment attenuates neuromuscular junction denervation, and axonal and motoneuron loss. DHT-treated SOD1-G93A mice demonstrates improvement in motor behavior as assessed by rota-rod and gait analyses, and an increased lifespan[2].

Protocol

Cell Research:

[1]
+ Expand
  • Cell lines: Bladder cancer cells
  • Concentrations: 1 nM
  • Incubation Time: 24 h
  • Method:

    Bladder cancer cells at a density of 50-60% confluence in 24-well plates are co-transfected with 250 ng of MMTV-luc reporter plasmid DNA and 2.5 ng of PRL-TK-luc plasmid DNA. After 6 h of transfection, the medium is replaced with another medium supplemented with charcoal-stripped FBS in the presence or absence of ligands (DHT, HF, or both) for 24 h. Cells were harvested, lysed, and assayed for luciferase activity.


    (Only for Reference)
Animal Research:

[2]
+ Expand
  • Animal Models: SOD1-G93A mutant mice with the congenic C57BL/6J background
  • Formulation: saline
  • Dosages: 5 mg
  • Administration: silastic implant
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (199.69 mM)
Ethanol 58 mg/mL (199.69 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 290.44
Formula

C19H30O2
CAS No. 521-18-6
Storage powder
in solvent
Synonyms androstanolone, stanolone, 5α-DHT

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04032067 Not yet recruiting Drug: GV1001 placebo|Drug: Proscar placebo Benign Prostatic Hyperplasia (BPH) GemVax & Kael August 28 2019 Phase 3
NCT03361969 Recruiting Drug: Estetrol|Drug: Placebo Oral Tablet Prostatic Neoplasm Pantarhei Oncology B.V. April 16 2018 Phase 2
NCT03314298 Completed Drug: testosterone anastrozole Mammographic Density Havah Therapeutics Pty Ltd August 14 2017 Phase 1
NCT02574910 Recruiting Drug: Abiraterone acetate Congenital Adrenal Hyperplasia University of Texas Southwestern Medical Center|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|University of Michigan|Children''s Hospital Los Angeles August 1 2017 Phase 1
NCT03085095 Recruiting Drug: Relugolix|Drug: Leuprolide Acetate Prostate Cancer Myovant Sciences GmbH April 18 2017 Phase 3
NCT02927210 Recruiting Drug: Dimethandrolone Undecanoate|Drug: Placebo Healthy Men|Male Contraception Health Decisions|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Lundquist Institute for Biomedical Innovation at Harbor-UCLA Medical Center|University of Washington December 2016 Phase 1

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID