Androgen Receptor

Principle

The androgen receptor (AR) plays a critical role in reproductive function, muscle growth, and is implicated in conditions such as prostate cancer. Upon activation by specific stimuli, AR translocates from the cytoplasm to the nucleus, where it binds to androgen response elements on DNA to regulate gene expression. Signosis has developed a stable AR luciferase reporter cell line in which luciferase activity directly reflects AR activation. This cell line serves as a robust reporter system for monitoring AR activation triggered by stimuli, gene overexpression, or gene knockdown.

The stable cell line was established by co-transfecting an AR luciferase reporter vector and a G418 resistance vector, followed by antibiotic selection. G418-resistant clones were screened for etoposide-induced luciferase activity, and the clone stably showing the highest induction was selected and expanded for our cell lines.

Applications

Prostate Cancer and Castration-Resistant Prostate Cancer (CRPC)

Signosis' AR luciferase reporter cell line is a powerful and versatile model for studying AR signaling in prostate cancer, including both hormone-sensitive and castration-resistant stages (CRPC). Since AR remains a central driver of tumor progression even after androgen deprivation therapy (ADT), our AR luciferase reporter cell lines are ideal for understanding the molecular mechanisms of disease progress and identifying effective treatment strategies for prostate cancer.

This model enables quantifiable measurement of AR transcriptional activity in response to pharmacological or genetic modulation. It supports a wide range of applications, including but not limited to:

Evaluating the efficacy of AR-targeted therapies such as enzalutamide, bicalutamide, and flutamide
Studying mechanisms of drug resistance including AR mutations or splice variant expression such as AR-V7
Screening novel small molecules or biologics that activate or inhibit AR function
Exploring cross-talk with key oncogenic pathways, including PI3K/AKT/mTOR, Wnt/β-catenin, and FOXA1

Common inducers and inhibitors that can be used with this model:

Dihydrotestosterone (DHT) or R1881 to activate AR signaling
Enzalutamide or flutamide as AR antagonists to inhibit AR function
AKT inhibitors (such as MK-2206) to explore compensatory survival pathways and synergy with AR inhibition

Signosis offers AR luciferase reporter cell line for high-throughput drug screening, combination therapy testing, and mechanistic research into AR-driven oncogenesis.

Endocrine Disruption and Environmental Toxicology

Signosis’ AR luciferase reporter cell line offers a reliable and high-throughput system for evaluating androgenic or antiandrogenic potential of environmental chemicals, industrial compounds, pharmaceuticals, and personal care products. Our cell lines are particularly suited for screening endocrine-disrupting chemicals (EDCs) that interact with AR, a key regulator of reproductive developmental and endocrine homeostasis.

By quantifying AR transcriptional activity through a sensitive luciferase readout, this system enables researchers to asses how test compounds influence AR activity. It is ideal for both academic and regulatory studies focused on chemical safety, reproductive toxicology, and hormone signaling. Such applications include:

Screening environmental or industrial chemicals (e.g., phthalates, bisphenols, pesticides) for androgenic or antiandrogenic activity
Evaluating pharmaceutical or cosmetic compounds for unintended endocrine effects
Characterizing dose-response and potency of known or novel EDCs
Comparing AR modulation alongside estrogen or glucocorticoid signaling pathways for full endocrine profiling

Common inducers and inhibitors that can be used with this model:

Dihydrotestosterone (DHT) or R1881 to activate AR signaling
Flutamide or cyproterone acetate as reference AR antagonists
BPA, vinclozolin, or linuron as test chemicals with known endocrine-disrupting effects

Signosis offers AR luciferase reporter cell line as a valuable tool for both mechanistic studies and high-throughput screening to meets the needs of toxicology researchers, regulatory labs, and safety assessors seeking fast, reproducible AR activity data.

Muscle Biology and related Disorders

Signosis’ AR luciferase reporter cell line is a valuable model for studying the roll of AR signaling in skeletal muscle physiology, growth, and regeneration. AR is known to play a critical role in muscle mass maintenance, and its activation is linked to anabolic effects on muscle tissue. This model provides a system to evaluate compounds with potential therapeutic effects for muscle-wasting conditions such as sarcopenia, cachexia, or age-related muscle loss.

By measuring AR-driven transcriptional activity, researchers can assess the anabolic potential of androgens, selective androgen receptor modulators (SARMs), and other small molecules targeting the AR pathway. Such applications include:

Evaluating SARMs or androgens for their ability to stimulate AR signaling relevant to muscle maintenance and regeneration
Screening therapeutic candidates for muscle-wasting disorders, including cancer cachexia and age-associated sarcopenia
Studying the impact of inflammation or glucocorticoids on AR signaling in muscle-related contexts
Exploring AR cross-talk with catabolic pathways such as FOXO, myostatin/SMAD, or inflammatory cytokines

Common inducers and inhibitors that can be used with this model:

Dihydrotestosterone (DHT) or R1881 to activate AR signaling
SARMs (e.g., LGD-4033, enobosarm) to assess tissue-selective AR activity
Dexamethasone or TNF-α to model catabolic or inflammatory suppression of AR signaling
Myostatin or TGF-β for pathway cross-talk studies

Signosis offers AR luciferase reporter cell line that enables reproducible analysis of AR activity for therapeutic development in the muscle and aging research fields.

Skin and Hair Biology

Signosis’ AR luciferase reporter cell line is a valuable tool for investigating AR signaling in the context of skin and hair biology, including conditions such as androgenetic alopecia, acne, and seborrheic dermatitis. Androgens, particularly dihydrotestosterone (DHT), play a pivotal role in regulating hair follicle cycling and sebaceous gland function via AR-mediated transcriptional programs.

By measuring AR-driven transcriptional activity, researchers can quantify AR activation or inhibition in response to pharmaceutical compounds, natural products, or environmental agents, making it practical for dermatological research and cosmetic development. Such applications include:

Screening topical agents or natural extracts for AR antagonistic or agonistic activity
Exploring cross-talk between AR and inflammatory or metabolic pathways in skin homeostasis

Common inducers and inhibitors that can be used with this model:

Dihydrotestosterone (DHT) or R1881 to activate AR signaling
Flutamide, spironolactone, or finasteride as AR pathway antagonists
Retinoic acid or pro-inflammatory cytokines (e.g., IL-1β, TNF-α) for cross-talk studies

Signosis offers fast and reproducible platforms for mechanistic studies and compound screening, supporting research in dermatology, cosmetology, and hair restoration.

Metabolism and Metabolic Pathway Studies

Signosis’ AR luciferase reporter cell line offers a targeted approach for studying AR involvement in metabolic reprogramming within cancer and hormone-responsive tissues. While not a whole-body metabolic model, this system is well-suited for dissecting AR-regulated metabolic gene networks, particularly those involved in lipid metabolism, oxidative stress, and tumor-associated energy shifts.

In AR-positive cancers such as triple-negative or apocrine-type breast cancer, AR signaling has been shown to influence lipid biosynthesis enzymes (e.g., FASN, SREBP1) and modulate oxidative stress pathways — key processes in metabolic adaptation and cancer cell survival. Such applications include:

Evaluating the metabolic impact of AR-targeting drugs on gene expression related to lipogenesis, redox balance, and energy metabolism
Screening small molecules or natural products for AR-dependent modulation of metabolic enzymes or stress response genes
Exploring AR cross-talk with metabolic pathways such as PI3K/AKT, mTOR, and AMPK
Investigating tumor-associated metabolic reprogramming driven by AR signaling in breast and hormone-related cancers

Common inducers and inhibitors used in these studies include:

Dihydrotestosterone (DHT) or R1881 to activate AR
Flutamide or enzalutamide to inhibit AR signaling
Fatty acid synthase inhibitors, mTOR inhibitors, or oxidative stress inducers to study metabolic cross-regulation

Signosis offers a fast and reproducible platform for mechanistic studies and compound screening, where AR activity intersects with metabolic gene regulation.

Benefits

High Sensitivity and Responsiveness

Each cell line is validated to induce a strong reporter signal in response to stimuli.

Consistent

The TF reporter construct is stably integrated into the genome to avoid cell-to-cell variations in experiments.

Efficient

Cell lines can be used right away for experiments to study different signaling pathways.

Mycoplasma Free

All cell lines have been tested negative for mycoplasma.

Products

AR Luciferase Reporter MDA-MB-453 Stable Cell Line SL-0008
Price$3,870.00

Quick Lead Time | Global Overnight Delivery Available

Purchase Order: info@signosisinc.com