Search Result
Results for "
Androgen receptor inhibitor
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-158102
-
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Others
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Cancer
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ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
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-
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- HY-164373
-
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Androgen Receptor
Apoptosis
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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 .
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-
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- HY-158102A
-
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Others
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Cancer
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ORIC-944 TFA is the TFA salt form of ORIC (HY-158102). ORIC-944 TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .
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-
-
- HY-136582
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Androgen receptor-IN-2
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Androgen Receptor
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Cancer
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Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer .
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-
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- HY-118409
-
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Androgen Receptor
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Endocrinology
Cancer
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VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .
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-
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- HY-131953
-
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Androgen Receptor
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Cancer
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Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM .
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-
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- HY-153772
-
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Androgen Receptor
|
Cancer
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Androgen receptor antagonist 8 (Example 13) is an androgen receptor antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research .
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-
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- HY-160221
-
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Androgen Receptor
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Cancer
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Androgen receptor degrader-4 (compound 99) is a select androgen receptor degrader with an IC50 value of 3 nM. Androgen receptor degrader-4 inhibits the proliferation of prostate cancer cells .
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-
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- HY-151220
-
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Androgen Receptor
|
Others
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Androgen receptor-IN-4 (Compound 206) is an androgen receptor inhibitor, and can be used for research of Kennedy's disease .
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-
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- HY-153276
-
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Androgen Receptor
|
Cancer
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Androgen receptor-IN-5 is an androgen receptor inhibitor with potent anticancer effects. Androgen receptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1) .
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-
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- HY-139623
-
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Androgen Receptor
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Cancer
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A4B17 is an androgen receptor N-terminal inhibitor for researching androgen-responsive prostate cancer.
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-
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- HY-155478
-
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Androgen Receptor
|
Cancer
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Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
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-
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- HY-152524
-
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Androgen Receptor
|
Cancer
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Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
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-
-
- HY-121094
-
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Estrogen Receptor/ERR
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Cancer
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Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
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-
-
- HY-105122
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WIN 49596
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Androgen Receptor
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Endocrinology
Cancer
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Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .
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- HY-15103
-
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Androgen Receptor
Thyroid Hormone Receptor
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Cancer
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AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) .
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-
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- HY-16079
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AZD3514
3 Publications Verification
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Androgen Receptor
|
Cancer
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AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
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-
-
- HY-143535
-
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Androgen Receptor
|
Cancer
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HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
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-
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- HY-117669
-
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Androgen Receptor
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Cancer
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VPC-14228 is a potent androgen receptor DNA binding domain (AR-DBD) inhibitor that interferes with the interaction of AR with androgen response elements and effectively blocks AR transcriptional activity. VPC-14228 can be used in prostate cancer research .
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-
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- HY-110028
-
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Cannabinoid Receptor
Fatty Acid Synthase (FASN)
Androgen Receptor
|
Endocrinology
Cancer
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Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis [2,3].
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-
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- HY-164371
-
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Androgen Receptor
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Cancer
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(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
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-
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- HY-160020
-
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Androgen Receptor
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Cancer
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ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
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-
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- HY-123308
-
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Androgen Receptor
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Cancer
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VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC50 of 0.31 µM. VPC13163 has anticancer effects .
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-
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- HY-111421
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-
-
- HY-N0790
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Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
|
Androgen Receptor
Apoptosis
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Cancer
|
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
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- HY-142923
-
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Androgen Receptor
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Cancer
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AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research .
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-
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- HY-N2345
-
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Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
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Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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-
-
- HY-124292
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Honokiol dichloroacetate
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Androgen Receptor
|
Cancer
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Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level .
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-
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- HY-N6714
-
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
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Infection
Cancer
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Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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-
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- HY-B0845
-
-
-
- HY-13613
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GG 745; GI 198745
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5 alpha Reductase
Apoptosis
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Cancer
|
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
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-
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- HY-103245
-
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Androgen Receptor
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Cancer
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Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
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-
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- HY-N0790R
-
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Androgen Receptor
Apoptosis
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Cancer
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Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
-
- HY-114246
-
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Others
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Cancer
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ONC1-13B is a potent androgen receptor (AR) antagonist with the activity of effectively inhibiting PSA expression in prostate cancer cells. ONC1-13B can effectively inhibit PSA expression and prostate cancer cell proliferation under DHT stimulation. ONC1-13B exerts its anti-tumor effect by preventing androgen from binding to AR and its nuclear translocation .
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-
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- HY-N7210
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Apoptosis
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Cancer
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Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
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- HY-163340
-
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Glucocorticoid Receptor
Androgen Receptor
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Cancer
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GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
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-
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- HY-156530
-
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Cytochrome P450
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Endocrinology
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CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer .
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-
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- HY-123163
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RWJ-66826; RTI-6617-003
|
Progesterone Receptor
Glucocorticoid Receptor
Androgen Receptor
Estrogen Receptor/ERR
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Endocrinology
Cancer
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JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
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-
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- HY-B0846
-
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Fungal
Androgen Receptor
Parasite
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Infection
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Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 µM .
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-
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- HY-N7045
-
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Androgen Receptor
Apoptosis
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Cancer
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Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
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-
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- HY-N2345R
-
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Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
|
Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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-
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- HY-B0845R
-
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Fungal
Estrogen Receptor/ERR
Androgen Receptor
Aryl Hydrocarbon Receptor
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Infection
Endocrinology
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Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM .
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-
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- HY-B0111
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Dihydrospirorenone
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Progesterone Receptor
Androgen Receptor
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Endocrinology
Cancer
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Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
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-
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- HY-156111
-
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PROTACs
Androgen Receptor
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Cancer
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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 .
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-
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- HY-141487
-
-
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- HY-109619
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Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
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Androgen Receptor
Cytochrome P450
|
Cancer
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
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-
-
- HY-N1943
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Δ13-Dehydrochaparrinone
|
Androgen Receptor
|
Inflammation/Immunology
Cancer
|
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
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-
-
- HY-118375
-
ISC-4
|
Apoptosis
|
Cancer
|
Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.
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-
-
- HY-149433
-
|
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 .
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-
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- HY-109070
-
EPI-002
|
Androgen Receptor
|
Cancer
|
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-13613R
-
GG 745 (Standard); GI 198745 (Standard)
|
5 alpha Reductase
Apoptosis
|
Cancer
|
Dutasteride (Standard) is the analytical standard of Dutasteride. This product is intended for research and analytical applications. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
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-
- HY-13613S
-
GG 745-13C6; GI 198745-13C6
|
Apoptosis
5 alpha Reductase
|
Cancer
|
Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
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-
- HY-153918
-
|
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 .
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-
- HY-158101
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CC-94676
|
Androgen Receptor
|
Cancer
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BMS-986365 (CC-94676) is an orally active and selective heterobifunctional ligand-directed degrader (LDD) targeting the androgen receptor (AR). BMS-986365 demonstrated significant in vivo potency, degrading AR, inhibiting AR signaling, and inhibiting tumor growth in animal models of advanced prostate cancer .
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- HY-B1866
-
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Androgen Receptor
|
Endocrinology
|
Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
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- HY-139970
-
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Androgen Receptor
|
Endocrinology
Cancer
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
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- HY-B0022
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Flutamide
Maximum Cited Publications
6 Publications Verification
SCH 13521
|
Androgen Receptor
|
Cancer
|
Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome .
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-
- HY-123875A
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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 .
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- HY-N7043
-
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Apoptosis
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Cancer
|
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
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- HY-164552
-
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Apoptosis
Androgen Receptor
|
Cancer
|
ZNU-IMB-Z15 (Compound Z15) is an antagonist and degrader of androgen receptor (AR). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive castration-resistant prostate cancer (CRPC) cell lines and induce their apoptosis, exhibiting anticancer activity both in vivo and in vitro .
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- HY-B0846S
-
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Fungal
Androgen Receptor
Parasite
|
Infection
|
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
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- HY-B0846R
-
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Fungal
Androgen Receptor
Parasite
|
Infection
|
Dimethomorph (Standard) is the analytical standard of Dimethomorph. This product is intended for research and analytical applications. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 µM .
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- HY-155543
-
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Androgen Receptor
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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 .
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- HY-121588
-
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Adrenergic Receptor
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Cancer
|
IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
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- HY-132292
-
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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 .
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-
- HY-13613S2
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GG 745-13C,15N,d; GI 198745-13C,15N,d
|
5 alpha Reductase
Apoptosis
Isotope-Labeled Compounds
|
Cancer
|
Dutasteride- 13C, 15N,d is 15N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
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-
- HY-147261
-
|
Histone Acetyltransferase
|
Cancer
|
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines .
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-
- HY-149914
-
|
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) .
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-
- HY-125065
-
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
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- HY-120018
-
|
Androgen Receptor
|
Cancer
|
VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.
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- HY-116501
-
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Androgen Receptor
|
Cancer
|
VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .
|
-
- HY-145709
-
|
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-100348
-
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
|
-
- HY-122611
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-122611A
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
|
-
- HY-N2908
-
Methyl atrarate
|
Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
|
Inflammation/Immunology
Cancer
|
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
|
-
- HY-B0022R
-
SCH 13521 (Standard)
|
Androgen Receptor
|
Cancer
|
Flutamide (Standard) is the analytical standard of Flutamide. This product is intended for research and analytical applications. Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome .
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- HY-B1866R
-
|
Androgen Receptor
|
Endocrinology
|
Linuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
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-
- HY-N7043R
-
|
Apoptosis
|
Cancer
|
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
|
-
- HY-162702
-
|
Androgen Receptor
PROTACs
|
Cancer
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 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 (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
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-
- HY-111784
-
Inobrodib
Maximum Cited Publications
6 Publications Verification
CCS1477
|
Epigenetic Reader Domain
|
Cancer
|
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
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-
- HY-113289
-
|
Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
|
-
- HY-124056
-
|
CXCR
|
Cancer
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-163940
-
|
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-116214
-
|
Fungal
Androgen Receptor
|
Infection
Endocrinology
|
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
- HY-100348R
-
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
|
-
- HY-116214S1
-
|
Isotope-Labeled Compounds
Fungal
Androgen Receptor
|
Infection
Endocrinology
|
Cyprodinil- 13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
- HY-116214R
-
|
Fungal
Androgen Receptor
|
Infection
Endocrinology
|
Cyprodinil (Standard) is the analytical standard of Cyprodinil. This product is intended for research and analytical applications. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
- HY-116214S
-
|
Isotope-Labeled Compounds
|
Others
|
Cyprodinil-d5is the deuterium labeledCyprodinil(HY-116214) . Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 μM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 μM) .
|
-
- 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 (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
|
-
- HY-B0561
-
SC9420
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
- HY-164477
-
|
Androgen Receptor
|
Cancer
|
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
|
-
- HY-N8504
-
NSC 260179; Spectinabilin
|
Bacterial
|
Infection
|
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50=13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50=1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s=34.3, 47, and 37.2 μg/mL, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50=0.84 μg/mL) and increases survival of P. densiflora trees inoculated with B. xylophilus.
|
-
- HY-160777
-
Galeterone 3β-imidazole
|
Androgen Receptor
MNK
|
Cancer
|
VNPP433-3β is a 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 inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
|
-
-
-
HY-L126
-
|
710 compounds
|
Nuclear receptors (NR) are proteins found in cells that sense androgen and thyroid hormones and certain other molecules. They are ligand-activated transcription factors that participate in many aspects of human physiology and pathology, and regulate the expression of various important genes.
Nuclear receptors have become one of the main targets in the development of new drug strategies, providing a unique type of receptors for studying a variety of human diseases, such as breast cancers, skin disorders and diabetes. 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors.
MCE supplies a unique collection of 710 nuclear receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on nuclear receptor. MCE Nuclear Receptor Library is a useful tool for drugs research related to cancer, skin disease and diabetes.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2413
-
|
Peptides
|
Others
|
Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-110028
-
-
-
- HY-N0790
-
-
-
- HY-N2345
-
-
-
- HY-N6714
-
-
-
- HY-N7045
-
-
-
- HY-N1943
-
-
-
- HY-N7043
-
-
-
- HY-N0790R
-
|
Triterpenes
Structural Classification
other families
Terpenoids
Source classification
Plants
|
Androgen Receptor
Apoptosis
|
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
|
-
-
- HY-N7210
-
|
Structural Classification
Natural Products
Source classification
Rubiaceae
Plants
Coffea arabica L.
|
Apoptosis
|
Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
|
-
-
- HY-N2345R
-
-
-
- HY-N2908
-
-
-
- HY-N7043R
-
-
-
- HY-113289
-
-
-
- HY-B0561
-
SC9420
|
Cardiovascular Disease
Classification of Application Fields
Disease Research Fields
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13613S
-
|
Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
|
-
-
- HY-B0846S
-
|
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
|
-
-
- HY-13613S2
-
|
Dutasteride- 13C, 15N,d is 15N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
|
-
-
- HY-116214S1
-
|
Cyprodinil- 13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
-
- HY-116214S
-
|
Cyprodinil-d5is the deuterium labeledCyprodinil(HY-116214) . Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 μM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 μM) .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-113289
-
|
|
Cholesterol
|
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
|
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