Search Result
Results for "
Androgens
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114612
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11-Oxotestosterone
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Androgen Receptor
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Endocrinology
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11-Ketotestosterone (11-Oxotestosterone), an oxidized form of Testosterone, is an active androgen .
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-
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- HY-113351
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-
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- HY-103246
-
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Androgen Receptor
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Cancer
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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 .
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- HY-122025
-
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Androgen Receptor
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Metabolic Disease
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AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
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- HY-139436
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-
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- HY-135732
-
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Androgen Receptor
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Cancer
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SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity .
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- HY-111044
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Androgen Receptor
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Cancer
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(+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases .
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- HY-103577
-
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Androgen Receptor
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Cancer
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LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM .
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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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- HY-106373
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ACTH; Adrenocorticotrophic hormone
|
Androgen Receptor
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Endocrinology
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Adrenocorticotropic hormone (ACTH) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production .
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-
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- HY-106373A
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ACTH TFA; Adrenocorticotrophic hormone TFA
|
Androgen Receptor
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Metabolic Disease
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Adrenocorticotropic hormone (ACTH) TFA is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production .
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- HY-157455
-
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Androgen Receptor
|
Cancer
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AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
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-
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- HY-160262
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-
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- HY-156751
-
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PROTACs
Androgen Receptor
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Cancer
|
PROTAC AR Degrader-6 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). PROTAC AR Degrader-6 blocks the process of androgen receptor transduction and also degrades the receptor itself. PROTAC AR Degrader-6 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975) .
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-
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- HY-14383
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-
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- HY-103578
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Androgen Receptor
|
Cancer
|
S-40503 is an orally active and selective androgen receptor modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone .
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- HY-B1623
-
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Estrogen Receptor/ERR
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Cancer
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Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer .
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-
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- HY-W653723
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NDCHA
|
Androgen Receptor
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Endocrinology
|
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
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- HY-131388
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-
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- HY-13607
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Androgen Receptor
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Cancer
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BMS-641988 (compound 23) is an oral active nonsteroidal androgen receptor antagonist with the Ki of 1.7 nM. BMS-641988 shows anticancer activity .
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- HY-70002B
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MDV3100 carboxylic acid
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Drug Metabolite
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Cancer
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Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist .
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- HY-123310
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Androgen Receptor
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Cancer
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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 .
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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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- HY-B1623R
-
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Estrogen Receptor/ERR
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Cancer
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Cyproterone (Standard) is the analytical standard of Cyproterone. This product is intended for research and analytical applications. Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer .
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- HY-W653723R
-
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Androgen Receptor
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Endocrinology
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N-Nitrosodicyclohexylamine (Standard) is the analytical standard of N-Nitrosodicyclohexylamine. This product is intended for research and analytical applications. N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
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- HY-14249
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Androgen Receptor
Autophagy
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Cancer
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Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .
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- HY-164807
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PROTACs
Androgen Receptor
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Cancer
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SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research .(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
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- HY-113603
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SPR001; LY2371712
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CRFR
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Cancer
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Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
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- HY-157491
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-
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- HY-108250
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Androgen Receptor
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Cancer
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(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .
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- HY-14249R
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Androgen Receptor
Autophagy
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Cancer
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Bicalutamide (Standard) is the analytical standard of Bicalutamide. This product is intended for research and analytical applications. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .
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- HY-160221
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PROTACs
Androgen Receptor
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Cancer
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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) .
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- HY-116501
-
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Androgen Receptor
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Cancer
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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 .
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- HY-133045
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-162702
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Androgen Receptor
PROTACs
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Cancer
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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-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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- HY-145709
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Androgen Receptor
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Cancer
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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) .
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- HY-164373
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Androgen Receptor
Apoptosis
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Cancer
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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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- HY-153342
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ARV-766
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PROTACs
Androgen Receptor
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Cancer
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Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
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- HY-138641
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ARV-110
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PROTACs
Androgen Receptor
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Cancer
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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)) .
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- HY-120018
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Androgen Receptor
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Cancer
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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-109070
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EPI-002
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Androgen Receptor
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Cancer
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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-115282A
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TRC-253
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Androgen Receptor
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Cancer
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JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-149862
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PROTACs
Androgen Receptor
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Cancer
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ARD-2051 is a potent 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 can be used for the research of prostate cancer .
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- 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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- HY-111309
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Androgen Receptor
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Endocrinology
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LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis .
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- HY-115282
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TRC-253 free base
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Androgen Receptor
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Cancer
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JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-100348
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Androgen Receptor
PPAR
Apoptosis
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Cancer
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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 .
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- HY-163940
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Aldose Reductase
Androgen Receptor
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Cancer
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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 .
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- HY-133044
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PROTAC Linkers
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Cancer
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Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-B0845
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- HY-145479
-
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PROTACs
Androgen Receptor
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Cancer
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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 .
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- HY-150102
-
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Androgen Receptor
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Cancer
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EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
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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-153772
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Androgen Receptor
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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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- HY-112689
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- HY-160659
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Androgen Receptor
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Endocrinology
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Androgen receptor antagonist 10 (compound 6h) is a androgen receptor antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model .
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- HY-133046
-
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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.
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- HY-146026
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities .
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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-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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- HY-169349
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
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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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- HY-146027
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .
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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
|
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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- HY-12111
-
-
- HY-151220
-
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Androgen Receptor
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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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- HY-146494
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
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- HY-155478
-
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Androgen Receptor
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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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- 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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- HY-153276
-
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Androgen Receptor
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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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- HY-162764
-
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Androgen Receptor
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Cancer
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Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
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- HY-152524
-
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Androgen Receptor
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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-113289
-
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Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
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Infection
Cardiovascular Disease
Neurological Disease
Cancer
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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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- 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-10561
-
PSK-3841; HMR-3841
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Androgen Receptor
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Endocrinology
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RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 has a dramatic effect on hair regrowth .
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- HY-130992
-
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Androgen Receptor
Ligands for Target Protein for PROTAC
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Cancer
|
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
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- HY-U00229
-
-
- HY-127057
-
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Androgen Receptor
CDK
MDM-2/p53
Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
|
Lambertianic acid is a bioactive diterpene with anti-allergic, antibacterial and anticancer activities. Lambertianic acid decreases androgen receptor protein levels, cellular and secretory levels of prostate-specific antigen. Lambertianic acid also suppresses cell proliferation by inducing G1 arrest, downregulating CDK4/6 and cyclin D1, activating p53, p21 and p27. Lambertianic acid induces Apoptosis and the expression of related proteins, including cleaved caspase-3/9, c-PARP and BAX, and inhibited BCl-2. Lambertianic acid is promising for research of prostate cancer .
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- HY-N9917
-
6′-O-Galloylalbiflorin
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Androgen Receptor
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Endocrinology
Cancer
|
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity .
|
-
- HY-16079
-
AZD3514
3 Publications Verification
|
Androgen Receptor
|
Cancer
|
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 .
|
-
- HY-113418
-
-
- HY-13702
-
Nilandron; RU 23908
|
Androgen Receptor
Parasite
|
Infection
Endocrinology
Cancer
|
Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties .
|
-
- HY-168141
-
|
Androgen Receptor
|
Cancer
|
Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC50=18 nM). .
|
-
- HY-107480
-
-
- HY-103576
-
-
- HY-114530
-
-
- HY-117669
-
|
Androgen Receptor
|
Cancer
|
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 .
|
-
- HY-135794
-
11-KDHT; 5α-Dihydro-11-keto testosterone
|
Androgen Receptor
|
Endocrinology
|
11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
|
-
- HY-15758
-
-
- HY-P1582
-
Adrenocorticotropic Hormone Fragment 1-14
|
Adrenergic Receptor
|
Cancer
|
ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
|
-
- HY-B0469
-
-
- HY-P1582A
-
Adrenocorticotropic Hormone Fragment 1-14 TFA
|
Adrenergic Receptor
|
Others
|
ACTH (1-14) (TFA) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production .
|
-
- HY-152850
-
|
Androgen Receptor
|
Endocrinology
Cancer
|
Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist .
|
-
- HY-117953
-
|
Prostaglandin Receptor
|
Endocrinology
|
RU 59063 is an N-substituted arylthiohydantoin compound with antiandrogenic activity and high relative binding affinity for the rat androgen receptor. RU 59063 is a nonsteroidal androgen receptor that functions as a radioactive AR radioprobe (Ki: 0.71 nM, rAR) when its trifluoromethyl group is replaced by a similar hydrophobic iodine atom .
|
-
- HY-13702R
-
|
Androgen Receptor
Parasite
|
Infection
Endocrinology
Cancer
|
Nilutamide (Standard) is the analytical standard of Nilutamide. This product is intended for research and analytical applications. Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties .
|
-
- HY-11027
-
-
- HY-18102A
-
-
- HY-N0790
-
Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
|
Androgen Receptor
Apoptosis
|
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) .
|
-
- HY-112257
-
S-23
1 Publications Verification
|
Androgen Receptor
|
Metabolic Disease
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .
|
-
- HY-135794R
-
|
Androgen Receptor
|
Endocrinology
|
11-Ketodihydrotestosterone (Standard) is the analytical standard of 11-Ketodihydrotestosterone. This product is intended for research and analytical applications. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
|
-
- HY-160692
-
|
Androgen Receptor
|
Others
|
AR antagonist 7 (86) is an androgen receptor (AR) antagonist that can be used in the research of hair loss .
|
-
- HY-105318
-
|
Androgen Receptor
|
Metabolic Disease
Endocrinology
|
LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction .
|
-
- HY-16060
-
ARN-509
|
Androgen Receptor
|
Cancer
|
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-U00323
-
2-Fluoro-7-[(3-pyridinyl)methyl]-9H-carbazole
|
Others
|
Endocrinology
|
Carbazole derivative 1 is a carbazole derivative which can be used to reduce androgen or oestrogen levels in mammals, including humans.
|
-
- HY-137448
-
SHR3680
|
Androgen Receptor
|
Cancer
|
Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer .
|
-
- HY-143535
-
|
Androgen Receptor
|
Cancer
|
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
|
-
- HY-13981
-
LGD-4033
|
Androgen Receptor
|
Endocrinology
|
Ligandrol (LGD-4033) is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.
|
-
- HY-120703
-
|
Androgen Receptor
|
Endocrinology
|
RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor .
|
-
- HY-15103
-
|
PTHR
Androgen Receptor
|
Cancer
|
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) .
|
-
- HY-14650
-
Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone
|
Androgen Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
Cancer
|
DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
|
-
- HY-112895
-
UT-155
2 Publications Verification
|
Androgen Receptor
|
Cancer
|
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
|
-
- HY-136596
-
|
Drug Metabolite
|
Cancer
|
Apalutamide-COOH is a metabolite of Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-162241
-
|
PROTACs
|
Others
|
SJH1-62B is a proteolysis targeting chimera (PROTAC) that can target the androgen receptor (AR) .
|
-
- HY-70002
-
Enzalutamide
Maximum Cited Publications
154 Publications Verification
MDV3100
|
Androgen Receptor
Autophagy
|
Cancer
|
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
|
-
- HY-16985
-
ODM-201; BAY-1841788
|
Androgen Receptor
|
Cancer
|
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
|
-
- HY-164371
-
|
Androgen Receptor
|
Cancer
|
(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
|
-
- HY-113415
-
-
- HY-110028
-
|
Cannabinoid Receptor
Fatty Acid Synthase (FASN)
Androgen Receptor
|
Endocrinology
Cancer
|
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].
|
-
- HY-15194
-
ASC-J9; GO-Y025
|
Androgen Receptor
|
Cancer
|
Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
|
-
- HY-N0790R
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
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-13604
-
|
Androgen Receptor
|
Endocrinology
Cancer
|
Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors .
|
-
- HY-112895A
-
|
Androgen Receptor
|
Cancer
|
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer .
|
-
- HY-111246
-
|
Androgen Receptor
|
Cancer
|
MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer .
|
-
- HY-123308
-
|
Androgen Receptor
|
Cancer
|
VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC50 of 0.31 µM. VPC13163 has anticancer effects .
|
-
- HY-163485
-
|
Androgen Receptor
|
Endocrinology
|
AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC50 of 0.76 μM .
|
-
- HY-B0891
-
17-Hydroxyprogesterone; 17-OHP
|
Progesterone Receptor
Endogenous Metabolite
|
Others
|
17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progesterone that serves as a chemical intermediate in the biosynthesis of other steroid hormones, including glucocorticoids, androgens, and estrogens.
|
-
- HY-N3755
-
|
Estrogen Receptor/ERR
|
Cancer
|
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .
|
-
- HY-107480R
-
|
Androgen Receptor
|
Metabolic Disease
|
YK11 (Standard) is the analytical standard of YK11. This product is intended for research and analytical applications. YK11 is a partial agonist of androgen receptor, with osteogenic activity.
|
-
- HY-114402
-
|
Androgen Receptor
PROTACs
|
Cancer
|
ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression . ARD-69 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-13331
-
Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-111421
-
-
- HY-W013249
-
|
PROTAC Linkers
|
Cancer
|
Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128 (HY-13229) .
|
-
- HY-W013272
-
HFT
|
Androgen Receptor
|
Cancer
|
Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer .
|
-
- HY-163813
-
-
- HY-106104
-
RU-38882; RU-882
|
Androgen Receptor
|
Inflammation/Immunology
Endocrinology
|
Inocoterone acetate (RU-38882) is a nonsteroidal antiandrogen. Inocoterone acetate binds to the androgen receptor and has antiandrogenic activity in animal models. Inocoterone acetate reduces inflammatory papules and pustules .
|
-
- HY-N6714
-
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
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 .
|
-
- HY-P2901
-
3α-HSD
|
Endogenous Metabolite
|
Endocrinology
|
3α-Hydroxysteroid Dehydrogenase, Microorganism (3α-HSD) is an enzyme encoded by the AKR1C4 gene, which can catalyze the conversion of 3-ketosteroids into 3α-hydroxy compounds. 3α-Hydroxysteroid dehydrogenase plays an important role in the inactivation of androgen DHT, and can convert DHT into 3α-androstanediol with weak androgen activity, which can be used in the research of hirsutism .
|
-
- HY-114246
-
|
Others
|
Cancer
|
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 .
|
-
- HY-18102
-
|
Androgen Receptor
|
Others
|
GLPG0492 is a non-steroidal selective androgen receptor modulator (potency 12 nM). GLPG0492 has the potential for the research of musculo-skeletal diseases such as sarcopenia and cachexia .
|
-
- HY-142923
-
|
Androgen Receptor
|
Cancer
|
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 .
|
-
- HY-B0469R
-
-
- HY-103687
-
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal agent, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-B1986
-
4,4'-DDE; p,p'-Dichlorodiphenyldichloroethylene
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
|
-
- HY-13273
-
MK-2866; GTX-024; Enobosarm
|
Androgen Receptor
|
Others
Cancer
|
Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism .
|
-
- HY-113415A
-
|
Endogenous Metabolite
Drug Metabolite
|
Endocrinology
|
Testosterone sulfate pyridinium is a Testosterone sulfate with a pyridinium. Testosterone sulfate is the metabolite of Testosterone. Testosterone is the main male sex hormone which determination is useful for assessment of androgen status .
|
-
- HY-164032
-
7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate
|
GnRH Receptor
|
Endocrinology
|
Dimethandrolone undecanoate (7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate) exhibits withrogens and progesterone activity. Dimethandrolone undecanoate inhibits production of gonadotropins, suppresses testosterone production, and thus inhibits sperm production. Dimethandrolone undecanoate is potent for development of male hormone contraceptives .
|
-
- HY-124292
-
Honokiol dichloroacetate
|
Androgen Receptor
|
Cancer
|
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 .
|
-
- HY-152512
-
|
Androgen Receptor
|
Cancer
|
RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
- HY-152520
-
|
Androgen Receptor
|
Cancer
|
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
- HY-13613
-
GG 745; GI 198745
|
5 alpha Reductase
Apoptosis
|
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 .
|
-
- HY-16060R
-
|
Androgen Receptor
|
Cancer
|
Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-N2345
-
|
Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-N6714R
-
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. 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 .
|
-
- HY-112256
-
ACP-105
5 Publications Verification
|
Androgen Receptor
|
Inflammation/Immunology
|
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
|
-
- HY-13607A
-
|
Androgen Receptor
|
Cancer
|
(rel)-BMS-641988 is a relative configuration of BMS-641988. BMS-641988 is a potent nonsteroidal androgen receptor antagonist. BMS-641988 has the potential for the research of prostate cancer .
|
-
- HY-N8856
-
|
Others
|
Others
|
Angelol M,isolated from the roots of Angelica gigas Nakai, shows activity in inhibiting prostate specific antigen (PSA) secreted from androgen dependent prostate cancer cell line, LNCaP cells .
|
-
- HY-15758R
-
|
Androgen Receptor
Autophagy
|
Cancer
|
3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
|
-
- HY-103245
-
|
Androgen Receptor
|
Cancer
|
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) .
|
-
- HY-16985R
-
|
Androgen Receptor
|
Cancer
|
Darolutamide (Standard) is the analytical standard of Darolutamide. This product is intended for research and analytical applications. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
|
-
- HY-70002R
-
|
Androgen Receptor
Autophagy
|
Cancer
|
Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
|
-
- HY-109564
-
|
Drug Metabolite
|
Cancer
|
5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.
|
-
- HY-130845
-
-
- HY-151266
-
|
Androgen Receptor
|
Cancer
|
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM .
|
-
- HY-114913
-
EL 222
|
Androgen Receptor
Bacterial
|
Infection
Endocrinology
|
Fenarimol (EL 222) is a potent and orally active fungicide. Fenarimol also is a androgen receptor inhibitor with an IC50 value of 19 µM. Fenarimol decreases the mRNA expression of PBP C3, ODC, IGF-1 .
|
-
- HY-111145
-
|
Androgen Receptor
|
Cancer
|
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
|
-
- HY-130845A
-
-
- HY-13604R
-
|
Androgen Receptor
|
Endocrinology
Cancer
|
Cyproterone acetate (Standard) is the analytical standard of Cyproterone acetate. This product is intended for research and analytical applications. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors .
|
-
- HY-158101
-
CC-94676
|
PROTACs
Androgen Receptor
|
Cancer
|
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .
|
-
- HY-125839
-
|
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
|
-
- HY-N7045
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
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 .
|
-
- HY-146397
-
|
PROTACs
Androgen Receptor
|
Cancer
|
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
|
-
- HY-P4413
-
|
Androgen Receptor
|
Endocrinology
|
(Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production .
|
-
- HY-P4456
-
|
Adrenergic Receptor
|
Endocrinology
|
(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production .
|
-
- HY-160680
-
|
Androgen Receptor
|
Endocrinology
|
AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model .
|
-
- HY-126464
-
EoM
|
Androgen Receptor
|
Cancer
|
Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC50 of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC50 of 9.73 μM .
|
-
- HY-W013272R
-
|
Androgen Receptor
|
Cancer
|
Hydroxyflutamide (Standard) is the analytical standard of Hydroxyflutamide. This product is intended for research and analytical applications. Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer .
|
-
- 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 .
|
-
- HY-19337
-
BAY 1896953; ORM-15341
|
Androgen Receptor
|
Endocrinology
|
Ketodarolutamide (ORM-15341) is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
|
-
- HY-148777
-
|
PROTACs
Androgen Receptor
|
Cancer
|
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP) .
|
-
- HY-N7210
-
|
Apoptosis
|
Cancer
|
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
-
|
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 .
|
-
- HY-12023
-
GTx-007
3 Publications Verification
S-4
|
Androgen Receptor
|
Cancer
|
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
|
-
- HY-109619
-
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
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.
|
-
- HY-N1943
-
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).
|
-
- HY-163641
-
|
Molecular Glues
Androgen Receptor
E1/E2/E3 Enzyme
|
Cancer
|
AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .
|
-
- 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.
|
-
- HY-15996
-
VT-464
|
Cytochrome P450
Androgen Receptor
|
Cancer
|
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
|
-
- HY-B0891S1
-
17-Hydroxyprogesterone-13C3; 17-OHP-13C3
|
Progesterone Receptor
Endogenous Metabolite
|
Others
|
17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
|
-
- HY-14250A
-
|
Androgen Receptor
|
Endocrinology
|
(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia .
|
-
- 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 .
|
-
- HY-Y0284
-
|
Others
|
Endocrinology
|
Diethyl phthalate is an endocrine disruptor that has the activity of affecting the apoptosis system of PC12 cells. Diethyl phthalate is widely used in a variety of plastics and personal care products. Diethyl phthalate has shown the potential to induce male reproductive toxicity unrelated to androgens in animal experiments .
|
-
- HY-13676
-
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-B0846
-
|
Fungal
Androgen Receptor
Parasite
|
Infection
|
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 .
|
-
- HY-114154
-
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity .
|
-
- 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].
|
-
- HY-B0561R
-
SC9420 (Standard)
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
|
Metabolic Disease
Cancer
|
Spironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
|
-
- HY-W753141
-
4,4'-DDE-13C12; p,p'-Dichlorodiphenyldichloroethylene-13C12
|
Isotope-Labeled Compounds
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
|
-
- HY-141487
-
-
- 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 .
|
-
- HY-B1986R
-
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
p,p'-DDE (Standard) is the analytical standard of p,p'-DDE. This product is intended for research and analytical applications. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
|
-
- HY-B1866
-
|
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 .
|
-
- HY-115747
-
|
Histone Demethylase
|
Cancer
|
Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research .
|
-
- HY-144127
-
|
Androgen Receptor
|
Cancer
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-139970
-
|
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) .
|
-
- 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-156530
-
|
Cytochrome P450
|
Endocrinology
|
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 .
|
-
- 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-B0022
-
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 .
|
-
- HY-123875A
-
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-N7043
-
|
Apoptosis
|
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 .
|
-
- HY-111372A
-
(Rac)-BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .
|
-
- HY-B1192
-
β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate
|
Estrogen Receptor/ERR
HBV
Bcl-2 Family
|
Neurological Disease
|
Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice .
|
-
- HY-B1805
-
3,4,4′-Trichlorocarbanilide
|
Bacterial
|
Infection
|
Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
|
-
- HY-14250
-
|
Androgen Receptor
|
Endocrinology
|
PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .
|
-
- HY-111614
-
|
Progesterone Receptor
|
Metabolic Disease
Cancer
|
Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity . Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research .
|
-
- HY-132292
-
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
|
-
- HY-130492
-
ARCC-4
1 Publications Verification
|
PROTACs
Androgen Receptor
|
Cancer
|
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .
|
-
- HY-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 .
|
-
- 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) .
|
-
- HY-163340
-
|
Glucocorticoid Receptor
Androgen Receptor
|
Cancer
|
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 .
|
-
- HY-N7045R
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
Isosilybin B (Standard) is the analytical standard of Isosilybin B. This product is intended for research and analytical applications. 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 .
|
-
- HY-155543
-
|
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-130431
-
|
Parasite
|
Infection
|
Vinclozolin M2 is an active metabolite of vinclozolin. It is formed from vinclozolin by successive esterase activity and decarboxylation of vinclozolin in C. elegans and by decarboxylation in human liver microsomes. Vinclozolin M2 is an antagonist of the mineralocorticoid receptor (IC50=1,400 nM) and androgen receptor (IC50=0.17 nM) in reporter assays using MCF-7 cells.
|
-
- HY-121588
-
|
Adrenergic Receptor
|
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 .
|
-
- HY-B0111
-
Dihydrospirorenone
|
Progesterone Receptor
Androgen Receptor
|
Endocrinology
Cancer
|
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. .
|
-
- HY-111024
-
PMC
|
Androgen Receptor
|
Cancer
|
2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines .
|
-
- HY-W748509
-
|
Caspase
Apoptosis
|
Cancer
|
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
|
-
- HY-13676R
-
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate (Standard) is the analytical standard of Megestrol acetate. This product is intended for research and analytical applications. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-B0846R
-
|
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 .
|
-
- HY-Y0284R
-
|
Apoptosis
|
Endocrinology
|
Diethyl phthalate (Standard) is the analytical standard of Diethyl phthalate. This product is intended for research and analytical applications. Diethyl phthalate is an endocrine disruptor that has the activity of affecting the apoptosis system of PC12 cells. Diethyl phthalate is widely used in a variety of plastics and personal care products. Diethyl phthalate has shown the potential to induce male reproductive toxicity unrelated to androgens in animal experiments .
|
-
- 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-111372
-
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- 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-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 .
|
-
- HY-B0022R
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SCH 13521 (Standard)
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Androgen Receptor
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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
-
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Androgen Receptor
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Endocrinology
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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 .
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-
- HY-106827
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RU 27987
|
Progesterone Receptor
Androgen Receptor
Phosphatase
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Endocrinology
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Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
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- HY-111614R
-
|
Progesterone Receptor
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Metabolic Disease
Cancer
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Melengestrol acetate (Standard) is the analytical standard of Melengestrol acetate. This product is intended for research and analytical applications. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity . Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research .
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-
- 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 .
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-
- HY-B1192R
-
|
Estrogen Receptor/ERR
HBV
Bcl-2 Family
|
Neurological Disease
|
Estradiol benzoate (Standard) is the analytical standard of Estradiol benzoate. This product is intended for research and analytical applications. Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice .
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-
- HY-135331
-
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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-
- HY-112083
-
|
AMPK
|
Cancer
|
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 μM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines .
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-
- 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))
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-
- 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-111784
-
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-111372R
-
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- HY-N6660
-
Tricaprin; Glyceryl tridecanoate
|
Endogenous Metabolite
Androgen Receptor
|
Cardiovascular Disease
Metabolic Disease
|
Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- HY-123163
-
RWJ-66826; RTI-6617-003
|
Progesterone Receptor
Glucocorticoid Receptor
Androgen Receptor
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
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) .
|
-
- HY-B1805S1
-
3,4,4'-Trichlorocarbanilide-13C13
|
Isotope-Labeled Compounds
Bacterial
|
Infection
|
Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
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-
- HY-122611R
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. 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
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-
- 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-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.
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-
- HY-133020
-
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-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-139659
-
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-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-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 .
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-
- HY-100186
-
|
Androgen Receptor
|
Cardiovascular Disease
Others
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
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-
- HY-149434
-
|
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 .
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-
- 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) .
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-
- 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-163784
-
|
Aldose Reductase
|
Cancer
|
AKR1C3-IN-14 (compound 4) is an AKR1C3 inhibitor (IC50=0.122 μM) that reduces the overproduction of androgens by inhibiting the activity of the AKR1C3 enzyme, thereby regulating hormone-mediated signaling. AKR1C3-IN-14 also plays a role in the biosynthesis of the prostaglandin PGF2α, regulating cell proliferation by affecting this pathway. AKR1C3-IN-14 can be used in the study of prostate cancer .
|
-
- HY-N6660R
-
|
Endogenous Metabolite
Androgen Receptor
|
Metabolic Disease
|
Trisdecanoin (Standard) is the analytical standard of Trisdecanoin. This product is intended for research and analytical applications. Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- 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-149127
-
ASC-JM17; ALZ-003
|
Keap1-Nrf2
Androgen Receptor
HSP
Mitophagy
|
Metabolic Disease
|
Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
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-
- 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.
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-
- HY-B0530A
-
γ-pipradol hydrochloride
|
Others
|
Cancer
|
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
|
-
- HY-160777
-
Galeterone 3β-imidazole
|
Molecular Glues
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-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-N3021
-
|
Endogenous Metabolite
NF-κB
TNF Receptor
FOXO
Microtubule/Tubulin
|
Metabolic Disease
|
D-chiro-Inositol is a stereoisomer of inositol that exhibits activities such as improving glucose metabolism, anti-tumor effects, anti-inflammatory properties, and antioxidant activity. D-chiro-Inositol effectively alleviates cholestasis by enhancing bile acid secretion and reducing oxidative stress. D-chiro-Inositol improves insulin resistance, lowers hyperglycemia and circulating insulin levels, reduces serum androgen levels, and ameliorates some metabolic abnormalities associated with X syndrome by mimicking the action of insulin. Additionally, D-chiro-Inositol can induce a reduction in pro-inflammatory factors (such as Nf-κB) and cytokines (such as TNF-α), thereby exerting anti-inflammatory effects. D-chiro-Inositol may be used in the study of liver cirrhosis, breast cancer, type 2 diabetes, and polycystic ovary syndrome .
|
-
- 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-L126
-
|
749 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 749 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-106373A
-
ACTH TFA; Adrenocorticotrophic hormone TFA
|
Androgen Receptor
|
Metabolic Disease
|
Adrenocorticotropic hormone (ACTH) TFA is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production .
|
-
- HY-P1582A
-
Adrenocorticotropic Hormone Fragment 1-14 TFA
|
Adrenergic Receptor
|
Others
|
ACTH (1-14) (TFA) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production .
|
-
- HY-106373
-
ACTH; Adrenocorticotrophic hormone
|
Androgen Receptor
|
Endocrinology
|
Adrenocorticotropic hormone (ACTH) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production .
|
-
- HY-P1582
-
Adrenocorticotropic Hormone Fragment 1-14
|
Adrenergic Receptor
|
Cancer
|
ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
|
-
- 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.
|
-
- HY-P4413
-
|
Androgen Receptor
|
Endocrinology
|
(Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production .
|
-
- HY-P4456
-
|
Adrenergic Receptor
|
Endocrinology
|
(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production .
|
-
- HY-P2446
-
APTAA-LHRH
|
Peptides
|
Endocrinology
|
ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-113351
-
-
-
- HY-113289
-
-
-
- HY-N9917
-
-
-
- HY-113418
-
-
-
- HY-15758
-
-
-
- HY-B0469
-
-
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- HY-N0790
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- HY-14650
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- HY-127057
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- HY-113415
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- HY-110028
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- HY-15194
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- HY-N0790R
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Triterpenes
Structural Classification
other families
Terpenoids
Source classification
Plants
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Androgen Receptor
Apoptosis
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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-B0891
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- HY-N3755
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- HY-N6714
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- HY-B0469R
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- HY-113415A
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- HY-N2345
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- HY-N6714R
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Structural Classification
Microorganisms
Source classification
Phenols
Polyphenols
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Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
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Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. 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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- HY-N8856
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- HY-15758R
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- HY-109564
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- HY-N7045
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- HY-N7210
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Structural Classification
Natural Products
Source classification
Rubiaceae
Plants
Coffea arabica L.
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Apoptosis
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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-N2345R
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- HY-N1943
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- HY-N7043
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- HY-B1192
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- HY-N7045R
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- HY-W748509
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- HY-N2908
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- HY-N7043R
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- HY-N6660
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Tricaprin; Glyceryl tridecanoate
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Ketones, Aldehydes, Acids
Source classification
umbellularia californica
Metabolic Disease
Plants
Lauraceae
Disease Research Fields
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Endogenous Metabolite
Androgen Receptor
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Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
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- HY-N6660R
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Ketones, Aldehydes, Acids
Source classification
umbellularia californica
Plants
Lauraceae
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Endogenous Metabolite
Androgen Receptor
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Trisdecanoin (Standard) is the analytical standard of Trisdecanoin. This product is intended for research and analytical applications. Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
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- HY-N3021
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Structural Classification
Natural Products
Classification of Application Fields
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
NF-κB
TNF Receptor
FOXO
Microtubule/Tubulin
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D-chiro-Inositol is a stereoisomer of inositol that exhibits activities such as improving glucose metabolism, anti-tumor effects, anti-inflammatory properties, and antioxidant activity. D-chiro-Inositol effectively alleviates cholestasis by enhancing bile acid secretion and reducing oxidative stress. D-chiro-Inositol improves insulin resistance, lowers hyperglycemia and circulating insulin levels, reduces serum androgen levels, and ameliorates some metabolic abnormalities associated with X syndrome by mimicking the action of insulin. Additionally, D-chiro-Inositol can induce a reduction in pro-inflammatory factors (such as Nf-κB) and cytokines (such as TNF-α), thereby exerting anti-inflammatory effects. D-chiro-Inositol may be used in the study of liver cirrhosis, breast cancer, type 2 diabetes, and polycystic ovary syndrome .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0891S1
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17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
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- HY-13613S
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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-W753141
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p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
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- HY-B1805S1
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Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
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- HY-116214S1
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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).
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Cat. No. |
Product Name |
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Classification |
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- HY-133020
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PROTAC Synthesis
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ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Cat. No. |
Product Name |
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Classification |
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- HY-113289
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Cholesterol
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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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