Androgen Receptor

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.

Protodioscin (Furostanol I) is a major steroidal saponin in dioscoreae rhizome, with anti-hyperlipidemia, anti-cancer properties.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]

Allura Red AC (CI 16035) is a very important food azo dye used in the food, pharmaceutical, paper, cosmetic and textile industries.Allura Red AC promotes susceptibility to experimental colitis via mouse intestinal serotonin.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

S-23 ((S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide) is an oral selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.

Testosterone Propionate is a short acting oil-based injectable formulation of testosterone. Testosterone inhibits gonadotropin secretion from the pituitary gland and ablates estrogen production in the ovaries, thereby decreasing endogenous estrogen levels.

Ostarine (MK-2866) is a non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Adrenosterone (11-ketoandrostenedione) is a steroid hormone isolated from the adrenal cortex.

AS-601811 is a steroidal 5α-reductase inhibitor and androgen receptor modulator used to study hair loss and acne.

JNJ-63576253 free base (TRC253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).

CTK8A3536 ((2-MORPHOLIN-4-YL-4-PHENYL-1,3-THIAZOL-5-YL)METHANOL) is an inhibitor of Androgen receptor.

BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer.

RU 59063 is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

3-[7 ,7- dimethyl-5-oxo -6H-pyrrolo[3,4-b]pyridin-2-yI]-1H-indole-7 -carbonitrile is an androgen receptor modulator.

MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is a selective androgen receptor modulator with an IC50 value of 6.6 nM for AR, which can be used for the prevention and treatment of cancer-related muscle wasting.

VPC-13566 is a BF3-specific small molecule, which effectively inhibited the androgen receptor transcriptional activity and displaced the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines and reduces the growth of AR-dependent prostate cancer xenograft tumors in mice.

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.

MK-0773 (PF-05314882) is a selective androgen receptor modulator that binds to AR (IC50: 6.6 nM) for the study of diseases caused by endocrine abnormalities.

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD).Ralaniten inhibits AR transcriptional activity with an IC50 value of 7.4 μM.Ralanites have anticancer activity and can be used to study desmoplasia-resistant prostate cancer (CRPC).

ONC1-13B is a potent androgen receptor (AR) antagonist with an ic50 in the range of 59-80 nM that inhibits PSA production in androgen-sensitive human PCa LNCaP cells.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

Epiandrosterone (EpiA) is a dehydroepiandrosterone metabolite and a precursor of testosterone and estradiol with hypolipidemic and anabolic property.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol), which has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.

Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).

Ailanthone (Δ13-Dehydrochaparrinone) is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69 nM) and constitutively active truncated AR splice variants (IC50: 309 nM).

Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR.

LGD-3303 is an orally available and selective androgen receptor modulator.

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1].

AC-262536 is a selective androgen receptor (SAR) modulator. It has partial agonist activity with respect to testosterone and suppresses luteinizing hormone.

ACP-105 is a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone.

BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer.

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

RAD140 is an investigational selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer.

p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT

N-Nitrosodicyclohexylamine (NDCHA), an N-nitrosocompound, exhibits anti-androgenic activity by competitively binding to the androgen receptor (AR) in opposition to 5α-dihydrotestosterone and reducing AR protein levels [1].

Nandrolone propionate is an anabolic steroid action primarily consisting of androgenic and nitrogen-retentive properties.

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor), prompting apoptosis in prostate cancer (PC) cells. In LNCaP xenograft models, BWA-522 demonstrated tumor growth inhibition (60 mg/kg, po; TGI=76%). The compound effectively reduced levels of AR-V7 and AR-FL by 77.3% at 1 μM and 72.0% at 5 μM, respectively, in VCaP and LNCaP cell lines [1].

Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex

Ligandrol is a novel nonsteroidal, oral SARM that binds to the androgen receptor with high affinity (Ki: 1 nM) and selectivity.

Ganoderic acid DM is an antiandrogenic osteoclastogenesis inhibitor, it especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1), this suppression leads to the inhibition of dendritic cell-specific transmembrane pr

(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, effectively downregulating androgen receptor expression by targeting both AR-FL mRNA and AR-V7 mRNA, with inhibition concentration (IC50) values of 3.1 μM and 5.5 μM, respectively [1].