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Ar-V7

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Aldose Reductase (2) Androgen Receptor (14) Apoptosis (9) c-Myc (1) DNA/RNA Synthesis (1) Fatty Acid Synthase (FASN) (1) Ligands for E3 Ligase (1) PARP (1) PROTACs (4)
By Research Areas:	Cancer (22)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145709

Ar-V7-IN-1	Androgen Receptor	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) .

HY-145479

*PROTAC AR-V7* degrader-1**	PROTACs Androgen Receptor	Cancer
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective *AR-V7* degrader with the DC₅₀ of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC₅₀ of 0.88 µM .

HY-148771

MTX-23 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-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-400766

BWA-522 intermediate-2	Others	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-123875A

Ralaniten triacetate EPI-506	Androgen Receptor	Cancer
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .

HY-147291

VPC-70063	c-Myc PARP Apoptosis	Cancer
VPC-70063 is a potent Myc-Max inhibitor with an IC₅₀ value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer .

HY-163510

*AR/AR-V7-IN-1*	Androgen Receptor	Cancer
AR/AR-V7-IN-1 (Compound 20i) is an *AR/ARV7* inhibitor (IC₅₀ = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC₅₀ values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .

HY-401056

BWA-522 intermediate-3	Others	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-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-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-161409

SC912	Androgen Receptor Apoptosis	Cancer
SC912 is an *AR-V7* inhibitor (IC₅₀ = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .

HY-139104

Thailanstatin D	DNA/RNA Synthesis Apoptosis	Cancer
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .

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-153918

(R)-SKBG-1	Androgen Receptor	Cancer
(R)-SKBG-1 is an RNA-binding protein NONO inhibitor. (R)-SKBG-1 suppresses androgen receptor expression with IC₅₀s of 3.1 μM and 5.5 μM against AR-FL mRNA and AR-V7 mRNA, respectively .

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-163940

LX1	Aldose Reductase Androgen Receptor	Cancer
LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and *AR-V7* and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .

HY-164373

SC428	Androgen Receptor Apoptosis	Cancer
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .

HY-155543

Anticancer agent 135	Androgen Receptor	Cancer
Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .

HY-163609

PROTAC AKR1C3 degrader-1	PROTACs Aldose Reductase	Cancer
PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .

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-124628

IPI-9119	Fatty Acid Synthase (FASN)	Cancer
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC₅₀ of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .

Thailanstatin D	Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields Cancer	DNA/RNA Synthesis Apoptosis
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .

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Ar-V7

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