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Results for "

LNCaP xenograft tumors

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

1

Peptides

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

    		PROTACs Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
    BWA-522
  • HY-149862
    ARD-2051
    1 Publications Verification

    		 PROTACs Androgen Receptor Cancer
    ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
    ARD-2051
  • 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-176128
    BWA-6047

    		PROTACs Androgen Receptor Apoptosis PARP Caspase Cancer
    BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
    BWA-6047
  • 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-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-178148
    AR antagonist 17

    		Androgen Receptor Endocrinology Cancer
    AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
    AR antagonist 17
  • 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-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-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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