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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> PARP

PARP

Poly (ADP-ribose) polymerases (PARPs) is a large family of proteins with a conserved catalytic domain that catalyze an immediate DNA-damage-dependent post-translational modification of histones and other nuclear proteins leading to the survival of injured proliferating cells. So far, a total number of 18 human PARP proteins encoded by different genes have been identified, including PARP-1 to PARP-4, PARP-5a, PARP-5b, PARP-5c and PARP-6 to PARP-16. The general structural of PARP proteins has been revealed through the extensive study of the founding family member PARP-1, which is characterized by the presence of four functional domains, including a DNA-binding domain, a caspase-cleaved domain, an automodification domain and a catalytic domain.

Products for  PARP

  1. Cat.No. Product Name Information
  2. GC11761 4-amino-1,8-Naphthalimide

    4-Aminonaphthalimide,4-ANI

     4-amino-1,8-Naphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells. 4-amino-1,8-Naphthalimide Chemical Structure
  3. GC35150 5,7,4'-Trimethoxyflavone 5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner. 5,7,4'-Trimethoxyflavone Chemical Structure
  4. GC68161 5-AIQ

    5-Aminoisoquinolin-1-one

     5-AIQ Chemical Structure
  5. GC73642 ALK-IN-26 ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 Chemical Structure
  6. GC70420 Amelparib Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib Chemical Structure
  7. GC70421 Amelparib hydrochloride Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride Chemical Structure
  8. GC65899 AZ3391 AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23). AZ3391 Chemical Structure
  9. GC16725 AZ6102 TNKS1/2 inhibitor AZ6102 Chemical Structure
  10. GC73919 AZD-9574-acid AZD-9574-acid (70D), a PPAR-1 inhibitor, can be used for the synthesis of PROTAC (CAS 2923686-70-6). AZD-9574-acid Chemical Structure
  11. GC73130 Basroparib

    STP1002

     Basroparib is a potent poly (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity. Basroparib Chemical Structure
  12. GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor Benzamide Chemical Structure
  13. GC14380 BGP-15 PARP inhibitor BGP-15 Chemical Structure
  14. GC35547 BR102375 BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%. BR102375 Chemical Structure
  15. GC33223 BRCA1-IN-1 BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively. BRCA1-IN-1 Chemical Structure
  16. GC35550 BRCA1-IN-2 BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions. BRCA1-IN-2 Chemical Structure
  17. GC68940 DB008

    DB008 is an effective selective inhibitor of PARP16 with an IC50 value of 0.27 μM and contains acrylamide electrophile. DB008 has membrane permeability and can selectively label PARP16.

     DB008 Chemical Structure
  18. GC64209 E7016

    GPI 21016

     E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent. E7016 Chemical Structure
  19. GC18172 E7449

    E7449; 2X-121

     E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM). E7449 Chemical Structure
  20. GC13541 G007-LK

    Tankyrase 1/2 Inhibitor VI

     tankyrase 1/2 inhibitor G007-LK Chemical Structure
  21. GC19542 GeA-69

    GeA-69 is a selective, highly cell permeable allosteric inhibitor

     GeA-69 Chemical Structure
  22. GC38385 INO-1001 INO-1001 Chemical Structure
  23. GC34195 K-756 K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively. K-756 Chemical Structure
  24. GC65907 KSQ-4279

    USP1-IN-1

     KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530). KSQ-4279 Chemical Structure
  25. GC13419 ME0328 PARP inhibitor,potent and selective ME0328 Chemical Structure
  26. GC12756 MK-4827 hydrochloride

    MK-4827 hydrochloride

     MK-4827 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. MK-4827 hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity. MK-4827 hydrochloride Chemical Structure
  27. GC11537 MK-4827 tosylate

    Niraparib tosylate

     MK-4827 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. MK-4827 tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity. MK-4827 tosylate Chemical Structure
  28. GC16914 MN 64 tankyrase inhibitor MN 64 Chemical Structure
  29. GC65202 Nesuparib

    JPI-547/OCN-201

     Nesuparib is a potent inhibitor of PARP. Nesuparib Chemical Structure
  30. GC34120 Niraparib R-enantiomer (MK 4827 (R-enantiomer))

    MK 4827 (R-enantiomer)

     Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM. Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Chemical Structure
  31. GC19264 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy. NMS-P118 Chemical Structure
  32. GC36751 NMS-P515 NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity. NMS-P515 Chemical Structure
  33. GC17555 NVP-TNKS656

    TNKS656

     TNKS2 inhibitor NVP-TNKS656 Chemical Structure
  34. GC69618 Olaparib-d8

    AZD2281-d8; KU0059436-d8

    Olaparib-d8 is the deuterated form of Olaparib (AZD2281). Olaparib is an orally effective PARP inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 5 and 1 nM, respectively. Olaparib is also an activator of autophagy and mitophagy.

     Olaparib-d8 Chemical Structure
  35. GC67906 OM-153 OM-153 Chemical Structure
  36. GC73184 OUL232 OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 Chemical Structure
  37. GC34071 Pamiparib (BGB-290)

    BGB-290

     Pamiparib (BGB-290) (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib (BGB-290) has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor. Pamiparib (BGB-290) Chemical Structure
  38. GC36855 Paris saponin VII Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia. Paris saponin VII Chemical Structure
  39. GC64579 PARP-1-IN-2 PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis. PARP-1-IN-2 Chemical Structure
  40. GC73272 PARP-1-IN-3 PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 Chemical Structure
  41. GC65927 PARP-2-IN-1 PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM. PARP-2-IN-1 Chemical Structure
  42. GC68006 PARP1-IN-11 PARP1-IN-11 Chemical Structure
  43. GC74078 PARP1-IN-29 PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 value of 6.3 nM. PARP1-IN-29 Chemical Structure
  44. GC69660 PARP1-IN-7

    PARP1-IN-7 is an inhibitor of poly ADP-ribose polymerase-1 (PARP1), used as an anticancer agent.

     PARP1-IN-7 Chemical Structure
  45. GC64578 PARP1-IN-8 PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-8 Chemical Structure
  46. GC69657 PARP10-IN-2

    PARP10-IN-2 is an effective inhibitor of mono-ADP-ribosyltransferase PARP10, with an IC50 of 3.64 μM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 27 μM and 11 μM for human PARP2 and human PARP15, respectively.

     PARP10-IN-2 Chemical Structure
  47. GC69658 PARP10-IN-3

    PARP10-IN-3 is a selective mono-ADP-ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 1.7 μM for both human PARP2 and human PARP15.

     PARP10-IN-3 Chemical Structure
  48. GC68035 PARP10/15-IN-1 PARP10/15-IN-1 Chemical Structure
  49. GC69655 PARP10/15-IN-2

    PARP10/15-IN-2 (Compound 8h) is an effective dual inhibitor of PARP10 and PARP15, with IC50 values of 0.15 μM and 0.37 μM, respectively. It can enter cells and prevent apoptosis.

     PARP10/15-IN-2 Chemical Structure
  50. GC69656 PARP10/15-IN-3

    PARP10/15-IN-3 (Compound 8a) is an effective dual inhibitor of PARP10 and PARP15, with IC50 values of 0.14 μM and 0.40 μM, respectively. It can enter cells and prevent apoptosis.

     PARP10/15-IN-3 Chemical Structure
  51. GC69659 PARP11 inhibitor ITK7

    ITK7

    PARP11 inhibitor ITK7 (ITK7) is an effective and selective inhibitor of PARP11. It can effectively inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for research on cellular localization.

     PARP11 inhibitor ITK7 Chemical Structure
  52. GC69661 PARP7-IN-14

    PARP7-IN-14 (I-1) is an effective selective PARP7 inhibitor with an IC50 value of 7.6 nM. PARP7-IN-14 has anti-cancer activity.

     PARP7-IN-14 Chemical Structure
  53. GC73566 PARP7-IN-15 PARP7-IN-15 (Compound 18) is a PARP7 inhibitor with IC50 of 0.56 nM, that has antitumor activity. PARP7-IN-15 Chemical Structure
  54. GC73639 PARP7-IN-16 PARP7-IN-16 (compound 36) is a potent, selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 Chemical Structure
  55. GC73640 PARP7-IN-16 free base PARP7-IN-16 free base is the free base form of PARP7-IN-16. PARP7-IN-16 free base Chemical Structure
  56. GC14251 Picolinamide poly (ADP-ribose) synthetase inhibitor Picolinamide Chemical Structure
  57. GC73943 Polθ/PARP-IN-1 Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 Chemical Structure
  58. GC65147 PROTAC PARP1 degrader PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM. PROTAC PARP1 degrader Chemical Structure
  59. GC69804 RBN-3143

    RBN-3143 is an effective NAD+ competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 is used for research on lung inflammation.

     RBN-3143 Chemical Structure
  60. GC72849 rel-PROTAC PARP1 degrader rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader. rel-PROTAC PARP1 degrader Chemical Structure
  61. GC19505 RK-287107

    RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively

     RK-287107 Chemical Structure
  62. GC13249 Rucaparib (free base)

    AG014447

     Rucaparib (free base) (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib (free base) is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib (free base) has the potential for castration-resistant prostate cancer (CRPC) research. Rucaparib (free base) Chemical Structure
  63. GC32793 Rucaparib Camsylate Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib Camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib Camsylate has the potential for castration-resistant prostate cancer (CRPC) research. Rucaparib Camsylate Chemical Structure
  64. GC67962 Simmiparib Simmiparib Chemical Structure
  65. GC69907 SK-575

    SK-575 is an efficient and specific protein-hydrolyzing targeted chimeric molecule (PROTAC) PARP1 degrader with an IC50 of 2.30 nM. SK-575 can effectively inhibit the growth of cancer cells carrying BRCA1/2 mutations.

     SK-575 Chemical Structure
  66. GC37728 Talazoparib tosylate

    BMN 673ts

     Talazoparib tosylate (BMN 673ts) is a potent and orally active PARP1/2 inhibitor, which is the tosylate salt form of Talazoparib. Talazoparib inhibits PARP1 with an IC50 value of 0.57 nM. Talazoparib tosylate Chemical Structure
  67. GC15041 Tankyrase Inhibitors (TNKS) 22

    TNKS 22;TNKS22;TNKS-22

     Tankyrase inhibitor Tankyrase Inhibitors (TNKS) 22 Chemical Structure
  68. GC11548 Tankyrase Inhibitors (TNKS) 49

    TNKS 49;TNKS49;TNKS-49

     Tankyrase inhibitor Tankyrase Inhibitors (TNKS) 49 Chemical Structure
  69. GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor Tankyrase-IN-2 Chemical Structure
  70. GC71552 TNKS-2-IN-1 TNKS-2-IN-1 (Compound 13g) is a TNKS-2 inhibitor. TNKS-2-IN-1 Chemical Structure
  71. GC73633 TNKS-2-IN-2 TNKS-2-IN-2 is a potent and selective inhibitor of TNKS2 with an IC50 of 22 nM. TNKS-2-IN-2 Chemical Structure
  72. GC73760 Trilexium

    TRX-E-009-1

     Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1. Trilexium Chemical Structure
  73. GC73136 VPC-70063 VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 Chemical Structure
  74. GC33358 WD2000-012547 WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221. WD2000-012547 Chemical Structure
  75. GC12781 XAV-939 XAV-939 selectively inhibits β-catenin-mediated transcription. XAV-939 Chemical Structure
  76. GC91435 YCH1899 YCH1899 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 It is selective for PARP1 and PARP2 over PARP3, -4, -5A, -5B, -6, -7, -10, and -12 (IC50s = 1-14.1 nM). YCH1899 Chemical Structure

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