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Androgenreceptor degrader-3 is an androgenreceptor degrader. Androgenreceptor degrader-3 blocks the process of androgenreceptor transduction and also degrades the receptor itself. Androgenreceptor degrader-3 can be used for prostate cancer research .
Androgenreceptor degrader-4 (compound 99) is a select androgenreceptor degrader with an IC50 value of 3 nM. Androgenreceptor degrader-4 inhibits the proliferation of prostate cancer cells .
Androgenreceptor-IN-6 (compound 16) is an orally available androgenreceptor (AndrogenReceptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgenreceptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
Androgenreceptor-IN-5 is an androgenreceptor inhibitor with potent anticancer effects. Androgenreceptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1) .
Androgenreceptor antagonist 8 (Example 13) is an androgenreceptor antagonist. Androgenreceptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgenreceptor antagonist 8 can be used for prostate cancer research .
Androgenreceptor antagonist 10 (compound 6h) is a androgenreceptor antagonist. Androgenreceptor antagonist 10 reduces the wax esters in the golden syrian hamster model .
Androgenreceptor antagonist 3 (Compound C18) is an androgenreceptor (AR) antagonist with an IC50 of 2.4 μM. Androgenreceptor antagonist 3 shows anticancer activities .
Masofaniten (Androgenreceptor-IN-2) is a potent and orally active androgenreceptor inhibitor. Masofaniten has antitumor activity against prostate cancer .
Androgenreceptor antagonist 4 (Compound AT2) is an androgenreceptor (AR) antagonist with an IC50 of 0.15 μM. Androgenreceptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgenreceptor antagonist 4 shows anticancer activities .
Androgenreceptor antagonist 5 (compound 42f) is a potent androgenreceptor (AR) antagonist with an IC50 value of 6.17 μM. Androgenreceptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgenreceptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgenreceptor antagonist 5 can be used for researching prostate cancer .
Androgenreceptor antagonist 7 is an effective androgenreceptor (AR) antagonist with an IC50 value of 1.18 µM. Androgenreceptor 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 .
Androgenreceptor antagonist 1 is an orally available full androgenreceptor (AR) antagonist with an IC50 of 59 nM . Androgenreceptor 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 .
TFM-4AS-1 is a selective androgenreceptor modulator (SARM). TFM-4AS-1 is a potent androgenreceptor (AR) ligand with an IC50 of 38 nm. TFM-4AS-1 is also a gene-selective agonist .
AC-262536 is a selective and non-steroidal androgenreceptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgenreceptor, with an affinity in the low nanomolar range (1-10 nM) .
AR antagonist 5 (compound 30a) is a selective androgenreceptor (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.
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgenreceptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
ABM-14 is a ligand for targeting androgenreceptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR .
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgenreceptor (AR) antagonist .
JNJ-26146900 is a potent and orally active androgenreceptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgenreceptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer .
ET516 is a potent inhibitor of AndrogenReceptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
Bavdegalutamide (ARV-110) is an orally active, specific androgenreceptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer .
K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgenreceptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgenreceptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgenreceptor (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 .
Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgenreceptor. 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) .
ARD-1676 is an orally available androgenreceptor (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 .
VPC-13566, a BF3-specific small molecule, is an androgenreceptor (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.
ARD-2051 is a potent and orally active androgenreceptor(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 .
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgenreceptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
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 androgenreceptor (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.
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 Androgenreceptor (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 .
EPI-7170, a ralaniten analogue, is a potent androgenreceptor 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) .
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 androgenreceptor (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.
Nilutamide (Nilandron) is an orally active nonsteroidal androgenreceptor antagonist with affinity for androgenreceptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties .
SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgenreceptor (AR) transcriptional activity .
AH3960 (compound 16c) is an antagonist of androgenreceptor. AH3960 binds wild as well as T877 mutant type androgenreceptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) .
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgenreceptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity .
RU 59063 is an N-substituted arylthiohydantoin compound with antiandrogenic activity and high relative binding affinity for the rat androgenreceptor. RU 59063 is a nonsteroidal androgenreceptor that functions as a radioactive AR radioprobe (Ki: 0.71 nM, rAR) when its trifluoromethyl group is replaced by a similar hydrophobic iodine atom .
S-23 is an orally active selective androgenreceptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgenreceptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .
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 androgenreceptor status. Leelamine hydrochloride suppresses transcriptional activity of androgenreceptor, which is known to regulate fatty acid synthesis [2,3].
AZD3514 is an orally activie and selective androgenreceptor (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 .
VPC-14228 is a potent androgenreceptor 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 .
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
Apalutamide-COOH is a metabolite of Apalutamide. Apalutamide is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgenreceptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors .
Dimethylcurcumin (ASC-J9) is an androgenreceptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
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, androgenreceptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity .
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 androgenreceptor (AR) antagonism .
Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors .
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 androgenreceptor (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 .
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 androgenreceptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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 .
ARD-69 (compound 34) is a potent PROTAC androgenreceptor degrader. ARD-69 induces degradation of androgenreceptor (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.
Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgenreceptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgenreceptor (AR) degrader ARD-2128 (HY-13229) .
Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgenreceptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer .
GLPG0492 is a non-steroidal selective androgenreceptor modulator (potency 12 nM). GLPG0492 has the potential for the research of musculo-skeletal diseases such as sarcopenia and cachexia .
Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgenreceptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
AR antagonist 2 (compound 58) is a potent androgenreceptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research .
Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .
AR/BET protein degrader-1 (Compound 149) is an AndrogenReceptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .
(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), androgenreceptor (AR), and progesterone receptor (>500-fold) .
Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgenreceptor (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 .
p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgenreceptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgenreceptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1].
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 androgenreceptor (AR) protein level .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 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 androgenreceptor (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[1][2].
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgenreceptor (AR) due to its structural similarity to DHT .
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
PF-998425 is a potent, selective nonsteroidal androgenreceptor (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 .
ACP-105 is an orally available, selective amd potent androgenreceptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
(rel)-BMS-641988 is a relative configuration of BMS-641988. BMS-641988 is a potent nonsteroidal androgenreceptor antagonist. BMS-641988 has the potential for the research of prostate cancer .
Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
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 androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Cl-4AS-1, a potent steroidal androgenreceptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
AR antagonist 1 (compound 29) is a potent androgenreceptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
AR antagonist 4 (Compound 67-b) is an orally active androgenreceptor (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 .
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), androgenreceptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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 androgenreceptor, dependent diseases and conditions, such as prostate cancer .
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgenreceptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
AR antagonist 1 (compound 29) hydrochloride is a potent androgenreceptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .
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 androgenreceptor (AR) degradation .
TD-802 (Compound 33c) is an androgenreceptor (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 .
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 androgenreceptor (AndrogenReceptor) 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 .
GA32 (compound 58r) is potent androgenreceptor (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 .
A031 is a highly effective PROTAC androgenreceptor (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) .
BMS-986365 is a selective heterobifunctional ligand-directed degrader (LDD) targeting the androgenreceptor (AR). BMS-986365 demonstrated significant in vivo potency, degrading AR, inhibiting AR signaling, and inhibiting tumor growth in animal models of advanced prostate cancer.
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). 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), androgenreceptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
GTx-007 (S-4) is an orally active and selective nonsteroidal androgenreceptor (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 .
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 androgenreceptor.
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgenreceptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651IC50=309 nM).
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgenreceptor (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. .
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgenreceptor-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) .
(Rac)-PF-998425 is a potent, selective, nonsteroidal androgenreceptor (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 .
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 androgenreceptor (AR) due to its structural similarity to DHT .
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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgenreceptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 µM .
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 androgenreceptor (AR) due to its structural similarity to DHT[2].
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgenreceptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM) . CLP-3094 is a selective, potent GPR142 antagonist .
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgenreceptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
(R)-SKBG-1 is an RNA-binding protein NONO inhibitor. (R)-SKBG-1 suppresses androgenreceptor expression with IC50s of 3.1 μM and 5.5 μM against AR-FL mRNA and AR-V7 mRNA, respectively .
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 androgenreceptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
AR antagonist 3 is a potent and selective androgenreceptor (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 .
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 androgenreceptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an AndrogenReceptor (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) .
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an AndrogenReceptor (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) .
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 androgenreceptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
Flutamide is an AndrogenReceptor 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 .
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgenreceptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
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-androgenreceptor (AR) axis .
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgenreceptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase) .
ARCC-4 is a low-nanomolar AndrogenReceptor (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 .
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgenreceptor (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) .
ARD-2128 is a highly potent, orally bioavailable PROTAC androgenreceptor (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 .
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgenreceptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations .
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 androgenreceptor-positive (AR+) prostate cancer cell lines .
WCA-814 is an androgenreceptor (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) .
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. 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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgenreceptor (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) .
VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgenreceptor (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 .
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 androgenreceptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines .
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. 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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgenreceptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgenreceptor) 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
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgenreceptor) 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
Atraric acid (Methyl atrarate) is a specific androgenreceptor (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 .
MK-4541 is an orally active and selective androgenreceptor (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 .
Flutamide (Standard) is the analytical standard of Flutamide. This product is intended for research and analytical applications. Flutamide is an AndrogenReceptor 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 .
ARD-61 is a highly potent, effective and specific PROTAC androgenreceptor (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.
EPI-001, a selective inhibitor of AndrogenReceptor (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 .
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 .
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgenreceptor 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 .
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 androgenreceptor (AR)- and C-MYC-regulated gene expression .
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgenreceptor 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 .
UT-34 is a potent, selective and orally active second-generation pan-androgenreceptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy .
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based AndrogenReceptor (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.
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 androgenreceptor (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).
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 AndrogenReceptor (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 .
GSK-2881078 is an orally active and nonsteroidal selective androgenreceptor 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 .
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the AndrogenReceptor 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 .
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgenreceptor 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 .
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 androgenreceptor (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).
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 androgenreceptor (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).
Cyprodinil-d5is the deuterium labeledCyprodinil(HY-116214) . Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgenreceptor (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) .
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 661 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.
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 androgenreceptor status. Leelamine hydrochloride suppresses transcriptional activity of androgenreceptor, which is known to regulate fatty acid synthesis [2,3].
Dimethylcurcumin (ASC-J9) is an androgenreceptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgenreceptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity .
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 androgenreceptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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 .
Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .
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 androgenreceptor (AR) degradation .
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgenreceptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651IC50=309 nM).
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-androgenreceptor (AR) axis .
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgenreceptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase) .
Atraric acid (Methyl atrarate) is a specific androgenreceptor (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 .
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgenreceptor 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 .
The androgen receptor protein is a steroid hormone receptor that acts as a ligand-activated transcription factor that regulates gene expression and affects cell proliferation and differentiation. Coactivators and corepressors such as ZBTB7A negatively regulate androgen receptor signaling by recruiting NCOR1 and NCOR2 to androgen response elements on target genes. Androgen receptor Protein, Human (His-SUMO) is the recombinant human-derived Androgen receptor protein, expressed by E. coli , with N-10*His, N-SUMO, C-Myc labeled tag. The total length of Androgen receptor Protein, Human (His-SUMO) is 369 a.a., with molecular weight of ~62.4 kDa.
The RNF14 protein is a critical E3 ubiquitin protein ligase that leads to activation of the RNF14-RNF25 translation quality control pathway during ribosome stalling. RNF14 is recruited by GCN1 to ubiquitinate and degrade translation factors, mainly EEF1A1/eEF1A, as well as ETF1/eRF1 and ribosomal proteins (RPL0, RPL1, RPL12, RPS13, RPS17). RNF14 Protein, Human is the recombinant human-derived RNF14 protein, expressed by E. coli , with tag free. The total length of RNF14 Protein, Human is 473 a.a., .
The RNF14 protein is a critical E3 ubiquitin protein ligase that leads to activation of the RNF14-RNF25 translation quality control pathway during ribosome stalling. RNF14 is recruited by GCN1 to ubiquitinate and degrade translation factors, mainly EEF1A1/eEF1A, as well as ETF1/eRF1 and ribosomal proteins (RPL0, RPL1, RPL12, RPS13, RPS17). RNF14 Protein, Human (His) is the recombinant human-derived RNF14 protein, expressed by E. coli , with N-6*His labeled tag. The total length of RNF14 Protein, Human (His) is 473 a.a., .
WDR77 is a non-catalytic component of the methylosome complex with PRMT5 and CLNS1A and regulates arginine to dimethylarginine in spliceosomal Sm proteins and histones. This modification directs Sm proteins to SMN complexes, helping them assemble into small nuclear ribonucleoprotein core particles. WDR77 Protein, Human (His-SUMO) is the recombinant human-derived WDR77 protein, expressed by E. coli , with N-His, N-SUMO labeled tag. The total length of WDR77 Protein, Human (His-SUMO) is 312 a.a., with molecular weight of ~49.6 kDa.
HIPK3; Homeodomain-interacting protein kinase 3; AndrogenReceptor-interacting nuclear protein kinase; ANPK; Fas-interacting serine/threonine-protein kinase; FIST; Homolog of protein kinase YAK1
HIPK3 is a multifaceted serine/threonine protein kinase that plays multiple roles in transcriptional regulation, apoptosis, and steroidogenic gene expression. It phosphorylates the transcription factors JUN and RUNX2, contributing to complex gene expression control. HIPK3 Protein, Human (Sf9, GST) is the recombinant human-derived HIPK3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of HIPK3 Protein, Human (Sf9, GST) is 402 a.a., .
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgenreceptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
Cyproterone acetate-d3 is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors[1][2].
Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgenreceptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1].
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 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 androgenreceptor (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[1][2].
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgenreceptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgenreceptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). 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), androgenreceptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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 androgenreceptor (AR) due to its structural similarity to DHT[2].
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgenreceptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. 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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. 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 androgenreceptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgenreceptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgenreceptor 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 .
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 androgenreceptor (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).
Cyprodinil-d5is the deuterium labeledCyprodinil(HY-116214) . Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgenreceptor (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) .
Androgen receptor Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 99 kDa, targeting to Androgen receptor. It can be used for WB,ICC/IF assays with tag free, in the background of Human.
RAN; ARA24; OK/SW-cl.81; GTP-binding nuclear protein Ran; AndrogenReceptor-associated protein 24; GTPase Ran; Ras-like protein TC4; Ras-related nuclear protein
RCHY1; ARNIP; CHIMP; PIRH2; RNF199; ZNF363; RING finger and CHY zinc finger domain-containing protein 1; AndrogenReceptor N-terminal-interacting protein; CH-rich-interacting match with PLAG1; E3 ubiquitin-protein ligase Pirh2; RING finger
WB
Human
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