Search Result
Results for "
androgen receptor (AR) ligand
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-103246
-
|
Androgen Receptor
|
Cancer
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist .
|
-
-
- HY-43962
-
-
-
- HY-131388
-
-
-
- HY-176347S
-
-
-
- HY-172954
-
-
-
- HY-170450
-
-
-
- HY-170330
-
-
-
- HY-173373
-
-
-
- HY-400666
-
-
-
- HY-400666A
-
-
-
- HY-156111
-
|
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-123310
-
|
Androgen Receptor
|
Cancer
|
JNJ-26146900 is a potent and orally active androgen receptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer .
|
-
-
- HY-170449
-
|
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-130845
-
-
-
- HY-130845A
-
-
-
- HY-111848A
-
|
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
-
|
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-173372
-
|
Androgen Receptor
PROTACs
|
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-138641
-
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-133045
-
|
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-170448
-
|
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-156751
-
(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-403733B
-
|
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-403733C
-
|
Androgen Receptor
|
Cancer
|
JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
|
-
-
- HY-403733A
-
|
Androgen Receptor
|
Cancer
|
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
|
-
-
- HY-169388
-
|
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-174391
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.
|
-
-
- HY-176068
-
|
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-169386
-
|
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-162702
-
|
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-114402
-
|
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 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).
|
-
-
- HY-160221
-
|
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-136242
-
|
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-149862
-
|
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-169387
-
|
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-161741
-
|
AUTOTACs
Androgen Receptor
|
Cancer
|
VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR +LC3 + autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer .(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
|
-
-
- HY-175455
-
|
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-170329
-
|
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-156751A
-
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-133046
-
|
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-164552
-
|
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-169385
-
|
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-159922
-
|
Androgen Receptor
|
Cancer
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
|
-
-
- HY-161369
-
|
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-176225
-
|
PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
|
|
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-176347S
-
|
Alpha Feto Protein, Arg- 13C36, 15N4, Lys- 13C6, 15N2 is the 13C- and 15N-labeled Alpha Feto Protein.
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-114402
-
|
|
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).
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: