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Results for "

enzalutamide

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

9

Peptides

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-70002
    Enzalutamide
    Maximum Cited Publications
    162 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 .
    Enzalutamide
  • HY-70002B
    Enzalutamide carboxylic acid
    1 Publications Verification

    MDV3100 carboxylic acid

    		 Drug Metabolite Cancer
    Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist .
    Enzalutamide carboxylic acid
  • HY-70002S1
    Enzalutamide-d6

    MDV3100-d6

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
    Enzalutamide-d6
  • HY-70002BS
    Enzalutamide carboxylic acid-d6

    MDV3100 carboxylic acid-d6

    		 Autophagy Androgen Receptor Isotope-Labeled Compounds Cancer
    Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
    Enzalutamide carboxylic acid-d6
  • HY-70002S
    Deutenzalutamide

    enzalutamide-d3; MDV3100-d3

    		 Androgen Receptor Autophagy Cancer
    Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
    Deutenzalutamide
  • HY-70002AS
    N-desmethyl Enzalutamide-d6

    N-desmethyl MDV 3100-d6

    		 Androgen Receptor Cancer
    N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
    N-desmethyl Enzalutamide-d6
  • HY-70002A
    N-desmethyl Enzalutamide

    N-desmethyl MDV 3100

    		 Androgen Receptor Cancer
    N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide .
    N-desmethyl Enzalutamide
  • HY-70002R
    Enzalutamide (Standard)

    		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 .
    Enzalutamide (Standard)
  • HY-70002BR
    Enzalutamide carboxylic acid (Standard)

    		Drug Metabolite Cancer
    Bromoxynil octanoate (Standard) is the analytical standard of Bromoxynil octanoate. This product is intended for research and analytical applications. Bromoxynil octanoate is an herbicide widely applied to maize, is potentially toxic to both animals and humans .
    Enzalutamide carboxylic acid (Standard)
  • HY-164371
    (+)-JJ-74-138

    		Androgen Receptor Cancer
    (+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
    (+)-JJ-74-138
  • HY-150102
    EPI-7170

    		Androgen Receptor Cancer
    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) .
    EPI-7170
  • 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 .
    ARCC-4
  • HY-163940
    LX1

    		Aldose Reductase Androgen Receptor Cancer
    LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .
    LX1
  • HY-164477
    FL442

    		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) .
    FL442
  • HY-163340
    GA32

    		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 .
    GA32
  • HY-121588
    IMTPPE

    		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 .
    IMTPPE
  • HY-159922
    AR antagonist 9

    		Androgen Receptor Cancer
    AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
    AR antagonist 9
  • HY-145388
    AU-15330
    5+ Cited Publications

    		 PROTACs Epigenetic Reader Domain Cancer
    AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
    AU-15330
  • HY-P4154
    Bevonescein

    ALM-488

    		 Fluorescent Dye Neurological Disease Cancer
    Bevonescein (ALM-488) is a novel, intravenously-administrated fluorescein-conjugated peptide that binds nerve-associated connective tissue, labels peripheral nerves under real-time fluorescence imaging (FL) in living mice and human ex vivo nerve tissue. Bevonescein is a peptide-linked tracer which fluorescently labeled both intact and degenerated nerves .
    Bevonescein
  • HY-155666
    YXG-158

    		Androgen Receptor Cancer
    YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .
    YXG-158
  • HY-P1103
    CTCE-9908
    1 Publications Verification

    		 CXCR Cancer
    CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
    CTCE-9908
  • HY-P1103A
    CTCE-9908 TFA

    		CXCR Cancer
    CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
    CTCE-9908 TFA
  • HY-P2231A
    Cotadutide acetate
    1 Publications Verification

    MEDI0382 acetate

    		 GCGR Metabolic Disease
    Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D) .
    Cotadutide acetate
  • HY-149408
    MAOA-IN-1

    		Monoamine Oxidase Cancer
    MAOA-IN-1 (compound 15) is an orally active MAOA inhibitor with cytotoxicity against prostate cancer cells. MAOA-IN-1 has Caco-2 permeability and lower CNS permeability. MAOA-IN-1 can be further used in the research of anti-cancer and anti-inflammatory indications .
    MAOA-IN-1
  • HY-118409
    VPC-3033

    		Androgen Receptor Endocrinology Cancer
    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) .
    VPC-3033
  • HY-P10026
    Nisotirostide

    LY-3457263

    		 Neuropeptide Y Receptor Metabolic Disease
    Nisotirotide (LY-3457263) is a PYY analog agonist studied in type 2 diabetes and obesity .
    Nisotirostide
  • HY-P4757
    N1-Glutathionyl-spermidine disulfide

    		Parasite Others
    N1-Glutathionyl-spermidine disulfide is a substrate of trypanothione reductase .
    N1-Glutathionyl-spermidine disulfide
  • HY-P2231
    Cotadutide
    1 Publications Verification

    MEDI0382

    		 GCGR Metabolic Disease
    Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D) .
    Cotadutide
  • HY-169385
    ATC-324

    		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).
    ATC-324
  • HY-136242
    UT-34

    		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.
    UT-34
  • HY-143471
    WNY0824

    PLK1/BRD4-IN-1

    		 Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Androgen Receptor c-Myc Cancer
    WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
    WNY0824
  • HY-P1321
    GR231118

    1229U91; GW1229

    		 Neuropeptide Y Receptor Neurological Disease
    GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
    GR231118
  • HY-P1321A
    GR231118 TFA

    1229U91 TFA; GW1229 TFA

    		 Neuropeptide Y Receptor Neurological Disease
    GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
    GR231118 TFA

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