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Androgen Receptor Degrader

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By Targets:	Androgen Receptor (50) Apoptosis (5) AUTACs (3) AUTOTACs (2) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (2) Estrogen Receptor/ERR (1) Histone Acetyltransferase (1) HSP (1) Keap1-Nrf2 (1) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (5) Mitophagy (1) MNK (1) Molecular Glues (3) Progesterone Receptor (1) PROTAC Linkers (2) PROTACs (26) SNIPERs (2)
By Research Areas:	Cancer (57) Endocrinology (4) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (3)

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Click Chemistry

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-164807

SARD279	PROTACs Androgen Receptor	Cancer
SARD279 is a potent and selective **Androgen Receptor** degrader with DC₅₀ value of 1099 nM. SARD279 can be used in prostate cancer research .(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))

HY-130992

Androgen receptor antagonist 1	Androgen Receptor Ligands for Target Protein for PROTAC	Cancer
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 .

HY-139436

ARD-2585	PROTACs Androgen Receptor	Cancer
ARD-2585 is an exceptionally potent and orally active PROTAC degrader of **androgen receptor** .

HY-162764

Androgen receptor degrader-5	Androgen Receptor	Cancer
Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior **androgen receptor** degradation activity and antiproliferative activity .

HY-160221

PROTAC AR Degrader-7	PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting **androgen receptor with an IC₅₀** value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305) .

HY-118409

VPC-3033	Androgen Receptor	Endocrinology Cancer
VPC-3033 is an **androgen receptor** antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC₅₀: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC₅₀=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .

HY-163813

AR Degrader-2	Molecular Glues Androgen Receptor	Cancer
AR Degrader-2 (Compound 2) is a molecular glue that degrades **androgen receptor (AR) with a DC₅₀** of 0.3-0.5 μM in cell VCaP.

HY-160262

AR/BET protein degrader-1	Androgen Receptor PROTACs Epigenetic Reader Domain	Cancer
AR/BET protein degrader-1 (Compound 149) is an **Androgen Receptor and BET** (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .

HY-170450

AR ligand-38	Androgen Receptor Ligands for Target Protein for PROTAC	Endocrinology
AR ligand-38 is the ligand for **androgen receptor*, that can be used for synthesis of PROTAC AR Degrader*-9 (HY-170448) .

HY-173626

EN1441	Androgen Receptor	Cancer
EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC₅₀ value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers .

HY-143535

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

HY-170330

AR ligand-33	Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
AR ligand-33 is the ligand for **androgen receptor*, that can be used for synthesis of PROTAC AR Degrader*-8 (HY-170329) as the target protein ligand .

HY-163641

AR Degrader-1	Molecular Glues Androgen Receptor E1/E2/E3 Enzyme	Cancer
AR Degrader-1 (Compound ML 2-9) is a molecular glue **androgen receptor** (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .

HY-15194

Dimethylcurcumin Maximum Cited Publications 14 Publications Verification ASC-J9; GO-Y025	Androgen Receptor	Cancer
Dimethylcurcumin (ASC-J9) is an **androgen receptor** degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.

HY-156751

(Rac)-GDC-2992 (Rac)-RO7656594; PROTAC AR Degrader-6	PROTACs Androgen Receptor	Cancer
(Rac)-GDC-2992 (Compound 1) is a PROTAC **androgen receptor** degrader (DC₅₀: 10 nM in VCaP cell). (Rac)-GDC-2992 blocks the process of androgen receptor transduction and also degrades the receptor itself. (Rac)-GDC-2992 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975) .

HY-111848A

PROTAC AR Degrader-4 TFA	SNIPERs PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an **Androgen Receptor** (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .

HY-111848

PROTAC AR Degrader-4	SNIPERs PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an **Androgen Receptor** (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .

HY-112895A

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

HY-170449

E3 ligase Ligand 48	Ligands for E3 Ligase	Others
E3 ligase Ligand 48 is a CRBN ligand for PROTAC AR Degrader-9 (HY-170448). PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for **androgen receptor*, that degrades* AR in human hair follicle papilla cells (HDPCs) with a DC₅₀ of 262.38 nM .

HY-W013249

Boc-piperazine-benzoic acid	PROTAC Linkers	Cancer
Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128 (HY-13229) .

HY-173372

PROTAC AR Degrader-10	Androgen Receptor	Cancer
PROTAC AR Degrader-10 is a protein degrader targeting the androgen receptor (AR) with a DC₅₀ value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .

HY-148777

A031	PROTACs Androgen Receptor	Cancer
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC₅₀ value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP) .

HY-156111

ARD-1676	PROTACs Androgen Receptor	Cancer
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .

HY-158101

BMS-986365 CC-94676	PROTACs Androgen Receptor	Cancer
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .

HY-173373

AR ligand-39	Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
AR ligand-39, an orally active and selective androgen receptor (AR) antagonist, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372) .

HY-131388

ABM-14	Ligands for Target Protein for PROTAC	Cancer
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 (HY-130492) to degrade AR .

HY-151266

AR antagonist 4	Androgen Receptor	Cancer
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC₅₀ of 246.6 nM against wt-AR, and is also an AR degrader with a DC₅₀ of 2.84 μM .

HY-176067

LO-4-25	Androgen Receptor	Cancer
LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its truncated variant AR-V7. LO-4-25 covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, promoting the ubiquitination of AR and AR-V7, which subsequently are recognized and degraded by the proteasome, reducing the protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research of androgen-independent prostate cancers .

HY-149862

ARD-2051	PROTACs Androgen Receptor	Cancer
ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC₅₀ values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer .

HY-146397

TD-802	PROTACs Androgen Receptor	Cancer
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .

HY-149433

BWA-522	Androgen Receptor Apoptosis	Cancer
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .

HY-130492

ARCC-4 1 Publications Verification	PROTACs Androgen Receptor	Cancer
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC₅₀ of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .

HY-138641

Bavdegalutamide 4 Publications Verification ARV-110	PROTACs Androgen Receptor	Cancer
Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986)) .

HY-170448

PROTAC AR Degrader-9	PROTACs Androgen Receptor	Endocrinology
PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for **androgen receptor*, that degrades* AR in human hair follicle papilla cells (HDPCs) with a DC₅₀ of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models . (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))

HY-157491

K2-B4-5e	PROTACs Androgen Receptor Epigenetic Reader Domain	Cancer
K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .

HY-132292

ARD-2128	PROTACs Androgen Receptor	Cancer
ARD-2128 is a highly potent, orally bioavailable *PROTAC androgen* receptor (AR)** degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .

HY-139659

ARD-61	PROTACs Androgen Receptor Progesterone Receptor Apoptosis	Cancer
ARD-61 is a highly potent, effective and specific *PROTAC androgen* receptor (AR)** degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133045

VHL Ligand 8	Ligands for E3 Ligase	Cancer
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM .

HY-169388

YT 6-2	AUTACs	Cancer
YT 6-2 is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen *Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation* effect on common AR mutants in PCa .

HY-149914

WCA-814	Androgen Receptor	Cancer
WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC₅₀: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .

HY-161369

CBPD-268	PROTACs Histone Acetyltransferase	Cancer
CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC₅₀ value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .

HY-169386

YT 6-2 analog-1	AUTACs	Cancer
YT 6-2 analog-1 (compound 2-3) is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen *Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation* effect on common AR mutants in PCa .

HY-153342

Luxdegalutamide 1 Publications Verification ARV-766	PROTACs Androgen Receptor	Cancer
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .

HY-136242

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-133020

ARD-266	PROTACs Androgen Receptor	Cancer
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based **Androgen Receptor** (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-169387

YT 6-2-PEG3-C2-NH2	AUTACs	Cancer
YT 6-2-PEG3-C2-NH2 is the p62/SQSTM1 targeting, autophagy-targeting ligand-linker conjugate of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen *Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation* effect on common AR mutants in PCa .

HY-170329

PROTAC AR Degrader-8	PROTACs Androgen Receptor Apoptosis	Cancer
PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for **androgen receptor** (AR), that degrades AR-FL with DC₅₀ of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC₅₀ of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC₅₀ of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model . (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))

HY-176068

3-Cl-Pyridine-amide-acrylaldehyde-piperazine	Androgen Receptor	Cancer
3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells .

HY-149434

PROTAC AR-NTD degrader 1	Androgen Receptor Apoptosis	Cancer
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .

HY-145479

PROTAC AR-V7 degrader-1	PROTACs Androgen Receptor	Cancer
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC₅₀ of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))

Cat. No.	Product Name		Classification

HY-139659

ARD-61		PROTAC Synthesis
ARD-61 is a highly potent, effective and specific *PROTAC androgen* receptor (AR)** degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133020

ARD-266		PROTAC Synthesis
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based **Androgen Receptor** (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the **androgen receptor*, which can induce androgen* receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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Androgen Receptor Degrader

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