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

GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.

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

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.

Ligandrol (LGD-4033) is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.

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) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism.

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.

MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an 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.