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(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts .
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) .
AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .
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 .
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) .
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone activates apoptotic protein in human lymphoma U937 cells[3]. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders[4][5].
Netarsudil hydrochloride (AR-13324 hydrochloride) is a Rho-associated protein kinas (ROCK) and norepinephrine transporter (NET) inhibitor. Netarsudil hydrochloride has effective in intraocular pressure (IOP) reduction .
ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities . ar-Turmerone activates apoptotic protein in human lymphoma U937 cells . ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders .
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .
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 ARprotein .
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
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 % ARprotein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces ARprotein, 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 androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations .
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .
BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
MRS5698 is a selective Giprotein-coupled A3 adenosine receptor(A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis .
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for ARprotein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP) .
SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .
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 .
(R)-SKBG-1 is an RNA-binding proteinNONO 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 .
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 ARprotein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
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.
MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
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 ARprotein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer .
Fluorogen binding modulator-1 (PubChem SID 125240934) is a fluorogen activating protein (FAP)-fluorogen binding modulator with -log EC50s of 6.61 and 6.37 for AM2.2-β2AR and AM2.2-GPR32, respectively .
BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .
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 .
K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and ARproteins in cells .
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor(AR) PROTAC degrader. ARD-266 effectively induces degradation of ARprotein 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.
BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding .
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 .
Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor(AR). SCH-202676 has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 µM .
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions .
Vasopressin Dimer (anti-parallel) TFA is an anti-parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (anti-parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor(AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
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 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[1][2].
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions .
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.
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 .
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.
MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.
Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions .
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions .
Vasopressin Dimer (anti-parallel) TFA is an anti-parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (anti-parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .
ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities . ar-Turmerone activates apoptotic protein in human lymphoma U937 cells . ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders .
EDNRA Protein, a receptor for endothelin-1, activates a phosphatidylinositol-calcium second messenger system through association with G proteins. Its binding affinities follow the order: ET1 > ET2 >> ET3. Additionally, EDNRA interacts with HDAC7 and KAT5. EDNRA Protein, Human (P.pastoris, His) is the recombinant human-derived EDNRA protein, expressed by P. pastoris , with N-His labeled tag. The total length of EDNRA Protein, Human (P.pastoris, His) is 60 a.a., with molecular weight of ~62 kDa.
Amphiregulin Protein, an EGFR ligand, serves as an autocrine growth factor and mitogen for various cells, including astrocytes, Schwann cells, and fibroblasts. It promotes cellular proliferation and interacts with CNIH in its immature precursor stage. Amphiregulin's EGFR activation underscores its role in essential cellular processes, emphasizing its significance as a regulator of cell growth and function in diverse cell types. Amphiregulin Protein, Human is the recombinant human-derived Amphiregulin protein, expressed by E. coli , with tag free. The total length of Amphiregulin Protein, Human is 98 a.a., with molecular weight of 14-16 kDa.
Amphiregulin Protein, an EGFR ligand, acts as an autocrine growth factor and mitogen for diverse cells, including astrocytes, Schwann cells, and fibroblasts. Engaging with CNIH in its immature stage, Amphiregulin's EGFR activation emphasizes its vital role in regulating cell growth and orchestrating various cellular functions across different cell types. Amphiregulin Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived Amphiregulin protein, expressed by HEK293 , with N-hFc labeled tag. The total length of Amphiregulin Protein, Mouse (HEK293, Fc) is 149 a.a., with molecular weight of 45-50 kDa.
The GRE3 protein is an aldose reductase that reduces the cytotoxic compound methylglyoxal (MG) to acetol and (R)-lactaldehyde, especially under stress conditions. MG is synthesized from dihydroxyacetone phosphate and is involved in cell cycle regulation and stress adaptation. GRE3 Protein, Saccharomyces cerevisiae is the recombinant GRE3 protein, expressed by E. coli , with tag free. The total length of GRE3 Protein, Saccharomyces cerevisiae is 327 a.a., .
EDNRA Protein, a receptor for endothelin-1, activates a phosphatidylinositol-calcium second messenger system through association with G proteins. Its binding affinities follow the order: ET1 > ET2 >> ET3. Additionally, EDNRA interacts with HDAC7 and KAT5. EDNRA Protein, Human (Cell-Free, His) is the recombinant human-derived EDNRA protein, expressed by E. coli Cell-free , with C-10*His labeled tag. The total length of EDNRA Protein, Human (Cell-Free, His) is 407 a.a., with molecular weight of 48.5 kDa.
The GRE3 protein is an aldose reductase that reduces the cytotoxic compound methylglyoxal (MG) to acetol and (R)-lactaldehyde, especially under stress conditions. MG is synthesized from dihydroxyacetone phosphate and is involved in cell cycle regulation and stress adaptation. GRE3 Protein, Saccharomyces cerevisiae (His) is the recombinant GRE3 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GRE3 Protein, Saccharomyces cerevisiae (His) is 327 a.a., .
Osteopontin/OPN Protein, a crucial non-collagenous bone protein, binds strongly to hydroxyapatite, integral to the mineralized matrix. It likely plays a vital role in mediating cell-extracellular matrix interactions. Moreover, as a cytokine, OPN efficiently induces interferon-gamma and interleukin-12 production while inhibiting interleukin-10, pivotal in promoting type I immunity. Osteopontin/OPN Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived Osteopontin/OPN protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of Osteopontin/OPN Protein, Mouse (P.pastoris, His) is 274 a.a., with molecular weight (glycosylation form) of ~60 kDa.
The C5AR2 protein is a receptor for C3a, C4a, and C5a peptides as well as ASP/C3adesArg, C4adesArg, and C5adesArg, and is weakly coupled to G(i)-mediated signaling pathways. It interacts with C3 and exhibits higher affinity for the lipogenic hormone ASP. C5AR2 Protein, Human (Cell-Free, His) is the recombinant human-derived C5AR2 protein, expressed by E. coli Cell-free , with C-10*His labeled tag. The total length of C5AR2 Protein, Human (Cell-Free, His) is 337 a.a., with molecular weight of 38.9 kDa.
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Mouse (HEK293, Fc) is a recombinant mouse IFNAR1 (E27-T429) with C-terminal hFc tag, which is produced in HEK293 cells.
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Mouse (HEK293, Fc) is a recombinant mouse IFNAR1 (E27-T429) with C-terminal His and Avi tags, which is produced in HEK293 cells.
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Human (HEK293, His-Avi) is a recombinant human IFNAR1 (K28-K436) with C-terminal His and Avi tag, which is produced in HEK293 cells.
ADORA2A Protein-VLP, a receptor for adenosine, activates adenylyl cyclase through G proteins. Its direct interaction with USP4 and GAS2L2 in the cytoplasmic C-terminal domain suggests regulatory roles. Interactions with DRD4 and NECAB2 imply involvement in diverse cellular signaling pathways. ADORA2A Protein-VLP, Human (HEK293) is the recombinant human-derived ADORA2A protein-VLP, expressed by HEK293, with tag free. The total length of ADORA2A Protein-VLP, Human (HEK293) is 412 a.a., with molecular weight of The target protein has a predicted MW of.
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Human (Biotinylated, HEK293, His-Avi) is a biotinylated recombinant human IFNAR1 (K28-K436) with C-terminal His and Avi tag, which is produced in HEK293 cells.
C5AR1 Protein-VLP, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays.
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone activates apoptotic protein in human lymphoma U937 cells[3]. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders[4][5].
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 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[1][2].
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