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PARP inhibitor resistance

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-161430

    DNA/RNA Synthesis Apoptosis Cancer
    RTx-161 is an allosteric Polθ polymerase inhibitor with an IC50 value of 4.1 nM. RTx-161 selectively kills HR-deficient cancer cells and suppresses PARP inhibitor (PARPi) resistance in multiple genetic backgrounds, including HR-proficient cells. Additionally, RTx-161 can induce apoptosis .
    RTx-161
  • HY-156498

    Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP Cancer
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
    RMC-7977
  • HY-123929

    MDM-2/p53 Wnt IKK Apoptosis Caspase Cancer
    PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
    PAWI-2
  • HY-161431

    DNA/RNA Synthesis Cancer
    RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells .
    RTx-152
  • HY-149348

    Topoisomerase PARP Apoptosis Cancer
    DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
    DiPT-4

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