ACP-105 is a novel non-steroidal SARM (Selective Androgen Receptor Modulator).

Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.

ASC-J9, is antitumor agent. ASC-J9 suppresses castration-resistant prostate cancer growth via degradation of full-length and splice variant androgen receptors.

AZD3514 is a potent and oral androgen receptor with Ki of 2.2 μM and has ability of reducing AR protein expression.

Boldenone undecylenate(Equipoise) is a synthetic steroid which has a similar effect as the natural steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans.

CB-03-01 is a steroidal ester, androgen antagonist derived from 11-deoxycortisone, which tightly mimics the profile of an ideal anti-androgen for topical use.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator

GSK2881078 (GSK-2881078 ) is a selective androgen receptor modulator (SARM).

LGD-4033 is a novel selective androgen receptor modulator (SARM)

MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

N-desmethyl Enzalutamide(N-desmethyl MDV3100) is a major metabolite of Enzalutamide, Enzalutamide(MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.

ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.

Ostarine(MK-2866; GTX-024)A modulator to human androgen receptor.

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).

RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM.

RU58841 is a nonsteroidal anti-androgen with potency (IC50 = 100 nM, Ka = 1.1 nM) comparable to hydroxyflutamide.

S23 is a novel Selective Androgen Receptor Modulator(SARM)

UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.

N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.

SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.

11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.

(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.

Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.

Bromopropylate is a pesticide with moderate anti-androgenic activities.

ABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 to degrade AR。

(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide. (R)-Bicalutamide is an androgen receptor (AR) antagonist, with an antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.

CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.

JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.

Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level.

Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).

Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer.

MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer.

A4B17 is an androgen receptor N-terminal inhibitor for treating androgen-responsive prostate cancer.

Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

(rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (rac)-PF-998425 has the potential for the research of the androgenetic alopecia.

HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43).

JNJ-pan-AR is a highly potent, selective antagonist of androgen receptor (AR) wild-type and F877L mutant for the treatment of the F877L mutant and wild-type CRPC.

VPC-13789 (VPC13789) is a potent, selective, orally available inhibitor of androgen receptor binding function-3 (BF3) site.VPC-13789 suppresses AR-mediated transcription, chromatin binding, and recruitment of coregulatory proteins.VPC-13789 selectively reduces the growth of both androgen-dependent and enzalutamide-resistant PCa cell lines.VPC-13789 demonstrated in vitro efficacy that reduced PSA production and tumor volume in animal models of CRPC with no observed toxicity.

Adrenocorticotropic hormone (ACTH) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production.

ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression.

EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC).

Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist.

RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castrated tolerant prostate cancer (mCRPC) cell line and can stably exist in vivo.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expre

Faznolutamide is a potent, selective androgen receptor (AR) antagonist.

JJ-450 is a novel analogue of IMTPPE and direct and specific inhibitor of androgen receptor (AR) transcriptional activity, blocks AR recruitment to androgen-responsive elements and suppresses AR target gene expression.

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.

A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM.

SC428 (SC-428) is a small molecule androgen receptor (AR) signaling inhibitor, directly binds to the AR N-terminal domain (NTD) and exhibits pan-AR inhibitory effect.

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).

UT-215 (UT215) is a small-molecule selective androgen receptor (AR) irreversible covalent antagonist, covalently and selectively bind to C406 and C327 in the AF-1 region of AR.

Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.