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Results for "

Androgen Receptor Degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (73) Adenosine Receptor (2) Akt (1) Aminopeptidase (2) Apoptosis (16) AUTACs (1) Autophagy (1) AUTOTACs (4) Calcium Channel (1) Caspase (2) Cytochrome P450 (3) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (2) Enteropeptidase (2) Epigenetic Reader Domain (2) ERK (2) Estrogen Receptor/ERR (2) Ferroptosis (1) GLUT (1) Histone Acetyltransferase (1) HSP (2) Keap1-Nrf2 (1) Ligands for E3 Ligase (3) Ligands for Target Protein for PROTAC (10) Mitochondrial Metabolism (1) Mitophagy (1) MNK (5) Molecular Glues (8) mTOR (2) Neprilysin (1) Opioid Receptor (2) p38 MAPK (1) Progesterone Receptor (1) Prostaglandin Receptor (1) PROTAC Linkers (2) PROTACs (34) Reactive Oxygen Species (ROS) (2) Reference Standards (1) SNIPERs (2) Src (1)
By Research Areas:	Cancer (82) Endocrinology (6) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (3)
Click Chemistry:	PROTAC Synthesis (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Click Chemistry

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-138641

Bavdegalutamide 5+ Cited Publications 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-158101

BMS-986365 1 Publications Verification CC-94676	PROTACs Androgen Receptor	Cancer
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC₅₀ of 10-40 nM). BMS-986365 is 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 no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .

HY-153342

Luxdegalutamide 2 Publications Verification ARV-766; JSB462	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-130492

ARCC-4 3 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-70006

Galeterone 3 Publications Verification TOK-001; VN-124-1	Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis	Cancer
Galeterone (TOK-001) is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research ^[1][2].

HY-15194

Dimethylcurcumin 10+ Cited Publications 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-156751A

GDC-2992 RO7656594	PROTACs Androgen Receptor	Cancer
GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC₅₀ value of 2.7 nM and inhibits proliferation with an IC₅₀ valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189A); Black: linker (HY-169975); E3 ligase ligand +linker (HY-169976A)) .

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-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-145479

PROTAC AR-V7 degrader-1 1 Publications Verification	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))

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-114402

ARD-69	PROTACs Androgen Receptor	Cancer
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 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).

HY-149433

BWA-522	PROTACs Androgen Receptor Apoptosis	Cancer
BWA-522 is an orally active PROTAC degrader targeting full-length **androgen receptor (AR-FL*) and androgen* receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .

HY-156111

ARD-1676 1 Publications Verification	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-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-170329

PROTAC AR Degrader-8	PROTACs Androgen Receptor Apoptosis	Cancer
PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC₅₀s 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 values 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. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .

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-160777

VNPP433-3β Galeterone 3β-imidazole	Molecular Glues Androgen Receptor MNK Apoptosis	Cancer
VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .

HY-149127

Rosolutamide ASC-JM17; ALZ-003	Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy	Metabolic Disease
Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant **androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis**, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .

HY-43962

Androgen receptor ligand 3	Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
Androgen receptor ligand 3 is an androgen receptor (AR) ligand. Androgen receptor ligand 3 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.

HY-139436

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

HY-149862

ARD-2051 1 Publications Verification	PROTACs Androgen Receptor	Cancer
ARD-2051 is a selective 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 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .

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-162702

AZ'3137	PROTACs Androgen Receptor	Cancer
AZ‘3137 is an orally active *PROTAC-type androgen* receptor (AR)** degrader with a DC₅₀ value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC₅₀ of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI₅₀ value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956) .

HY-175652

AZD9750	PROTACs Adenosine Receptor	Cancer
AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR ^L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .

HY-164552

ZNU-IMB-Z15	Apoptosis Androgen Receptor	Cancer
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .

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-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-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-175455

LYA914	PROTACs Androgen Receptor Akt	Cancer
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .

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-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-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-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-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-169387

YT 6-2-PEG3-C2-NH2	AUTOTACs	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-70006A

Galeterone hydrochloride TOK-001 hydrochloride; VN-124-1 hydrochloride	Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis	Cancer
Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research ^[1][2].

HY-133046

VHL Ligand-Linker Conjugates 17	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 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-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-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-177694

PROTAC AR Degrader-11	PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-11 is a potent **androgen receptor** and androgen receptor splice variant-7 PROTAC degrader. PROTAC AR Degrader-11 shows potent cytotoxicity against both CWR22RV1 cells and VCaP cells. PROTAC AR Degrader-11 can be used in prostate cancer research . (Structure Note: Pink: Androgen Receptor ligand (HY-171809); Blue: CRBN ligand (HY-A0003); Black: linker (HY-169966))

HY-171809

AR ligand 42	Ligands for Target Protein for PROTAC Androgen Receptor	Endocrinology
AR ligand 42 is a **androgen receptor** ligand. AR ligand 42 can be used to synthesize androgen receptor PROTAC degrader ITRI-90 (HY-171808) .

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-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-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-174377

PeS-9	Androgen Receptor p38 MAPK Caspase Cytochrome P450 Calcium Channel Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism GLUT	Cancer
PeS-9 is an **Androgen Receptor** (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors .

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))

Cat. No.	Product Name

HY-L935

Molecular Glue POI binding Fragment library

1039 compounds

POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases.

This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets.

MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.

Cat. No.	Product Name	Target	Research Area

HY-P11642A

Sialorphin TFA	Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor	Inflammation/Immunology
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

HY-P11642

Sialorphin	ERK Androgen Receptor Opioid Receptor Enteropeptidase mTOR Aminopeptidase	Neurological Disease Inflammation/Immunology Cancer
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

Cat. No.	Product Name		Classification