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PARP

PARP inhibitors block poly(ADP-ribose) polymerases (PARPs), enzymes that mark DNA damage and recruit repair proteins. PARP1 and PARP2 bind DNA single-strand breaks and attach poly(ADP-ribose) chains to themselves and to nearby chromatin proteins. Cells lacking breast cancer susceptibility proteins 1 or 2 (BRCA1, BRCA2), and therefore defective in homologous recombination, are highly sensitive to PARP inhibition. This synthetic lethal relationship, reported in 2005, has shaped much of the research on DNA repair inhibitors. Olaparib, niraparib, veliparib and talazoparib target the catalytic domains of PARP1 and PARP2, and 3-aminobenzamide is an early benzamide inhibitor. XAV 939 instead inhibits tankyrases 1 and 2 (TNKS1, TNKS2), which stabilizes axin in Wnt signaling studies.

Items 251-252 of 252

  • PARP1-IN-56
    Cat. No.
    B22007
    CAS No.
    1574367-80-8

    PARP1-IN-56

    PARP1-IN-56 is a potent inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), a key enzyme involved in DNA repair mechanisms. This compound can be radiolabeled with isotopes such as 211At or 125I, facilitating its application as an α-emitting radiotherapeutic agent in oncological research. PARP1-IN-56 has significant potential for studying cancer therapy by targeting PARP1's role in tumor survival and proliferation.

    In stock View Details
    5 mg
    $445.00
    10 mg
    $720.00
    All 2 sizes
  • MC2050
    Cat. No.
    B22026
    CAS No.
    1301757-19-6

    MC2050

    MC2050 is a selective inhibitor of PARP-1, exhibiting an IC50 of 119 nM. This compound effectively reduces hyperactivation of PARP-1 prompted by oxidative stress and lowers the levels of poly(ADP-ribosyl)ation on histone H1. MC2050 demonstrates protective effects against oxidative stress-mediated cell death in neuroblastoma cells induced by hydrogen peroxide. It is particularly valuable for research in the areas of neuroblastoma and Burkitt lymphoma.

    In stock View Details
    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 251-252 of 252

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