Search Result

Pathways Recommended:	PROTAC

Results for "

AR PROTAC degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (12) PROTAC Linkers (5) ADC Linker (1) Adenosine Receptor (1) Adrenergic Receptor (2) Akt (1) Androgen Receptor (41) Apoptosis (11) Caspase (2) Drug Intermediate (2) E3 Ligase Ligand-Linker Conjugates (4) Epigenetic Reader Domain (2) Estrogen Receptor/ERR (3) Histone Acetyltransferase (2) HSP (1) Ligands for E3 Ligase (5) MDM-2/p53 (1) PARP (1) Progesterone Receptor (1) PROTACs (41) PSMA (1) RAR/RXR (1) SNIPERs (2) Src (2) SWI/SNF Complex (1)
By Research Areas:	Cancer (65) Endocrinology (3) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (3)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Targets Recommended: PROTAC-Linker Conjugates for PAC PROTAC Linkers Ligands for Target Protein for PROTAC

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-145388

AU-15330 Maximum Cited Publications 11 Publications Verification	PROTACs SWI/SNF Complex	Cancer
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .

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-148771

MTX-23 1 Publications Verification PROTAC AR-V7 degrader-2	PROTACs Androgen Receptor Apoptosis	Cancer
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis .

HY-158113

CBPD-409	Histone Acetyltransferase PROTACs	Cancer
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC₅₀ of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC₅₀s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .

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-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-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-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-162412

PROTAC AR/AR-V7 degrader-1	PROTACs Adrenergic Receptor Apoptosis	Cancer
PROTAC AR/AR-V7 degrader-1 (27c) is a *PROTAC*-based and dual AR, AR-V7 degrader, with DC₅₀ values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .

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-30756

tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate	PROTAC Linkers	Others
tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate is a PROTAC linker. tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate can be used in the synthesis of PROTAC ER Degrader-12 (HY-160264) and PROTAC AR Degrader-9 (HY-170332) .

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-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-111846

PROTAC ERα Degrader-2 1 Publications Verification	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .

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-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-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-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-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-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-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-179433

PROTAC AR Degrader-12	PROTACs Androgen Receptor Estrogen Receptor/ERR Src	Cancer
PROTAC AR Degrader-12 is a highly efficient *PROTAC* targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .

HY-160547

PROTAC AR Degrader-5	PROTACs Androgen Receptor	Metabolic Disease
PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC₅₀ value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration (Pink: ligand for target protein (HY-169967); black: linker (HY-169966); Blue: E3 ligase ligand (HY-125845)) .

HY-147100

α1A-AR Degrader 9c	PROTACs Adrenergic Receptor	Cancer
α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible *α1A-AR* (Adrenergic receptor) PROTAC degrader, with a DC₅₀ of 2.86 μM. α1A-AR Degrader 9c induces *α1A-AR* degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC₅₀ of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research .

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-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-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-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-W877989

BWA-522 intermediate-1	Ligands for E3 Ligase	Cancer
BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .

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-176128

BWA-6047	PROTACs Androgen Receptor Apoptosis PARP Caspase	Cancer
BWA-6047 is an oral active *PROTAC* degrader targeting *AR/AR-V7* and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .

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-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-149434

PROTAC AR-NTD degrader 1	Androgen Receptor PROTACs 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-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-179056

Psa-AR	PROTACs PSMA Androgen Receptor HSP Apoptosis	Cancer
Psa-AR is a PROTAC degrader targeting PSMA, with a K_d of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer .

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-400766

BWA-522 intermediate-2	Drug Intermediate	Cancer
BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .

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-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-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-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-173372

PROTAC AR Degrader-10	Androgen Receptor PROTACs	Cancer
PROTAC AR Degrader-10 (GT19) 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-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-W041652

5-Hydroxypentanoic acid	ADC Linker	Cancer
5-Hydroxypentanoic acid is a PROTAC linker. 5-Hydroxypentanoic acid can be used in the synthesis of PROTAC AR-V7 degrader-1 (HY-145479) .

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) .

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library

94 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 94 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Cat. No.	Product Name		Classification

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 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-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.

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