Search Result

Results for "

AR and AR-V7 degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Linker (1) Adrenergic Receptor (1) Akt (1) Androgen Receptor (20) Apoptosis (11) AUTACs (1) AUTOTACs (3) Bcl-2 Family (1) c-Myc (1) Caspase (3) CDK (2) Drug Intermediate (2) E1/E2/E3 Enzyme (1) EGFR (1) HSP (3) Ligands for E3 Ligase (1) MDM-2/p53 (1) Molecular Glues (3) PARP (1) Prostaglandin Receptor (1) PROTACs (11) PSMA (1) RAR/RXR (1)
By Research Areas:	Cancer (29) Endocrinology (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-W854844B

JP-2-196 hydrochloride	Molecular Glues E1/E2/E3 Enzyme	Cancer
JP-2-196 hydrochloride is a covalent molecular glue degrader targeting RNF126. JP-2-196 hydrochloride induces the formation of a ternary complex between RNF126 and target proteins (e.g., BRD4, AR-V7), promoting their ubiquitination and proteasomal degradation. JP-2-196 hydrochloride is promising for research of cancers (e.g., prostate cancer, leukemia) .

HY-178938

AR Degrader-3	Molecular Glues Androgen Receptor Caspase Apoptosis	Endocrinology Cancer
AR Degrader-3 is an orally active molecular glue that targets *AR/ARV7* and induces the degradation of AR and *ARV7* through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .

HY-169385

ATC-324	AUTOTACs Androgen Receptor	Cancer
ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. 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 . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).

HY-181727

AR/AR-V7 degrader-1	Androgen Receptor HSP CDK	Cancer
AR/AR-V7 degrader-1 is an orally active AR and *AR-V7* degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .

HY-170820

XYD049	Molecular Glues Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc	Cancer
XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC₅₀ of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, *AR-V7, PSA* and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .

HY-401056

BWA-522 intermediate-3	Drug Intermediate	Cancer
BWA-522 intermediate-3 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-169386

YT 6-2 analog-1	AUTOTACs	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-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-182331

WCF-598	PROTACs RAR/RXR Androgen Receptor Apoptosis Caspase MDM-2/p53	Cancer
WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces *AR-V7* degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates *AR-V7* levels, and inhibits the transcription of downstream target genes of *AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53* signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer .

HY-403733B

(+)-JJ-450	Androgen Receptor Prostaglandin Receptor	Cancer
(+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .

HY-171808

ITRI-90	Androgen Receptor PROTACs Apoptosis	Cancer
ITRI-90 is an orally active androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades both full-length AR (AR-FL) and the splice variant AR-V7 protein via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the target gene expression. ITRI-90 significantly inhibits the proliferation of prostate cancer cells and induces apoptosis, include Enzalutamide-resistant growth cell. ITRI-90 exhibits favorable pharmacokinetic properties and demonstrates potent antitumor efficacy in vivo. ITRI-90 can be used for prostate cancer research .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.

AR and AR-V7 degrader

Inhibitors & Agonists