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PARP - PARP1

Poly(ADP-ribose) polymerase 1 (PARP1) is a crucial DNA repair enzyme that plays a key role in the cellular response to DNA damage. It catalyzes poly(ADP-ribosyl)ation (PARylation), a post-translational modification that regulates DNA repair, gene expression, and cell survival. DNA Damage-Dependent PARylation Process by PARP1 The activation of PARP1 and its PARylation reaction is a multi-step process, which includes: DNA Damage Recognition Upon single-strand breaks (SSBs) or double-strand breaks (DSBs), PARP1 binds to damaged DNA via its zinc finger domains (Zn fingers). This binding induces a conformational change that activates its catalytic domain. NAD⁺ Binding and Hydrolysis Activated PARP1 utilizes NAD⁺ (nicotinamide adenine dinucleotide) as a substrate. It cleaves NAD⁺ to release nicotinamide and generate an ADP-ribose unit. Attachment of ADP-Ribose Monomers The initial ADP-ribose unit is covalently attached to PARP1 itself or other target proteins, such as histones and DNA repair factors. Poly(ADP-Ribose) Chain Elongation PARP1 continues to catalyze the transfer of multiple ADP-ribose units, forming linear or branched poly(ADP-ribose) (PAR) chains. This modification recruits DNA repair complexes, facilitating base excision repair (BER) and homologous recombination (HR). Regulation of Target Proteins PAR chains act as a platform for protein-protein interactions, modulating DNA repair, chromatin remodeling, and transcriptional regulation. PARP1 Auto-Regulation and PAR Degradation Once DNA repair is complete, poly(ADP-ribose) glycohydrolase (PARG) degrades PAR chains. This restores cellular homeostasis and prevents excessive PARP1 activity.
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  1. A10019
    A-966492

    PARP1 inhibitor

    A-966492 displayed high potency against the poly(ADP-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay.
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  2. A10045
    Rucaparib (AG-014699) phosphate

    PARP inhibitor

    AG-014699 (Rucaparib) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.
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  3. A10046
    AG14361

    PARP1 inhibitor

    AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.
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  4. A10111
    Olaparib (AZD2281)

    PARP inhibitor

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
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  5. A10164
    BSI-201 (Iniparib)

    PARP1 inhibitor

    BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.
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  6. A11026
    MK-4827 (Niraparib)

    PARP inhibitor

    MK-4827 is a novel potent, orally bioavailable PARP-1 and PARP-2 inhibitor.
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  7. A11243
    Talazoparib (BMN673)

    PARP inhibitor

    BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
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  8. A12393
    AZD-2461

    PARP Inhibitor

    AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein.
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  9. A12665
    PJ 34 hydrochloride

    PARP inhibitor

    PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).
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  10. A14182
    Rucaparib

    PARP-1 inhibitor

    Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells.
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  11. A14371
    TAK1/MAP4K2 inhibitor 1

    PARP-1 inhibitor

    TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.

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  12. A15024
    BMN-673 8R,9S

    PARP Inhibitor

    BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673. BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM.
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  13. A15215
    PJ34

    PARP inhibitor

    PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.
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  14. A15371
    BYK 204165

    PARP-1 inhibitor

    BYK204165 is a cell-permeable isoquinolinedione compound that potently and selectively inhibits poly (ADP-ribose) polymerase 1 (PARP1).
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  15. A15372
    BYK 49187

    PARP-1/PARP-2 inhibitor

    BYK 49187, PARP-1 and PARP-2 inhibitor (pIC50 values are 8.36 and 7.50 for cell-free recombinant PARP-1 and murine PARP-2 respectively).
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  16. A15373
    DR 2313

    PARP inhibitor

    PARP Inhibitor XIDR 2313, PARP Inhibitor XI, is a water soluble pyrimidinone compound that functions as a PARP (Poly(ADP-ribose) polymerase) inhibitor.
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  17. A15374
    EB-47 dihydrochloride

    PARP1 Inhibitor

    EB 47 is a potent inhibitor of PARP1 with IC50 of 45 nM.
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  18. A15927
    MN-64

    TNKS inhibitor

    MN-64 is a potent and selective inhibitor of Tankyrase 1 and 2 (IC50 = 6 and 72 nM, respectively).
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  19. A16618
    Niraparib tosylate

    PARP1/PARP2 inhibitor

    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.
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  20. A18013
    Rucaparib Camsylate

    PARP inhibitor

    Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1, and also shows binding affinity to eight other PARP domains.
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  21. A18018
    Niraparib hydrochloride

    PARP1 and PARP2 inhibitor

    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
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  22. A18449
    NMS-P515

    PARP-1 inhibitor

    NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays.
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  23. A19092
    Tankyrase-IN-2

    Tankyrase inhibitor

    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively).
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  24. A20238
    Talazoparib tosylate

    PARP1/2 inhibitor

    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
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  25. A20994
    NMS-P118

    PARP-1 Inhibitor

    NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
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  26. A21356
    Veliparib dihydrochloride

    PARP inhibitor

    Veliparib dihydrochloride is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
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  27. A21553
    Stenoparib (E7449)

    PARP1/PARP2 inhibitor

    E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ?50 and ?50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
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  28. A21880
    Niraparib R-enantiomer

    PARP1 inhibitor

    Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
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