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Results for "

LNCaP xenograft

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149433
    BWA-522

    		Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
    BWA-522
  • HY-144127
    AR antagonist 3

    		Androgen Receptor Cancer
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
    AR antagonist 3
  • HY-121065
    BN-82685

    IRC-083065

    		 Phosphatase Cancer
    BN-82685 is a a quinone-based CDC25 inhibitor with IC50 of 201 nM, 117 nM, 109 nM, 160 nM, 249 nM, for CDC25C, CDC25C-cat, CDC25A, CDC25B2, CDC25B3, respectively. BN-82685 plays an important role in cancer research .
    BN-82685
  • HY-160777
    VNPP433-3β

    Galeterone 3β-imidazole

    		 Molecular Glues Androgen Receptor MNK Cancer
    VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
    VNPP433-3β
  • HY-P10816
    PACE4 Inhibitory peptide C23

    Ac-(DLeu)LLLRVK-Amba

    		 Bacterial Infection Cancer
    PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
    PACE4 Inhibitory peptide C23
  • HY-146494
    Androgen receptor antagonist 5

    		Androgen Receptor Cancer
    Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
    Androgen receptor antagonist 5
  • HY-169078
    ML234

    		Histone Methyltransferase Cancer
    ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
    ML234
  • HY-170951
    AR antagonist 10

    		Androgen Receptor Cancer
    AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .
    AR antagonist 10
  • HY-163608
    Ac-macropa

    		PSMA Cancer
    Ac-macropa is a PSMA-targeted Actinium-225 Conjugate, and can be used for study of prostate cancer .
    Ac-macropa
  • HY-163510
    AR/AR-V7-IN-1

    		Androgen Receptor Cancer
    AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
    AR/AR-V7-IN-1
  • HY-163612
    XY077

    		ROR Apoptosis Cancer
    XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
    XY077
  • HY-163611
    XY039

    		ROR Cancer
    XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
    XY039
  • HY-149091
    KDM5B-IN-4

    		Histone Demethylase Cancer
    KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
    KDM5B-IN-4
  • 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

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