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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-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-AIQ  Chemical Structure
  5. 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
  6. GC16725 AZ6102 TNKS1/2 inhibitor AZ6102  Chemical Structure
  7. GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor Benzamide  Chemical Structure
  8. GC14380 BGP-15 PARP inhibitor BGP-15  Chemical Structure
  9. 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
  10. 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
  11. 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
  12. GC64209 E7016 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
  13. GC18172 E7449 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
  14. GC13541 G007-LK tankyrase 1/2 inhibitor G007-LK  Chemical Structure
  15. GC19542 GeA-69

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

    GeA-69   Chemical Structure
  16. GC38385 INO-1001 INO-1001  Chemical Structure
  17. 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
  18. GC65907 KSQ-4279 KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530). KSQ-4279  Chemical Structure
  19. GC13419 ME0328 PARP inhibitor,potent and selective ME0328  Chemical Structure
  20. GC12756 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
  21. GC11537 MK-4827 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
  22. GC16914 MN 64 tankyrase inhibitor MN 64  Chemical Structure
  23. GC65202 Nesuparib Nesuparib is a potent inhibitor of PARP. Nesuparib  Chemical Structure
  24. GC34120 Niraparib 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
  25. GC19264 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy. NMS-P118  Chemical Structure
  26. 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
  27. GC17555 NVP-TNKS656 TNKS2 inhibitor NVP-TNKS656  Chemical Structure
  28. GC69618 Olaparib-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
  29. GC67906 OM-153 OM-153  Chemical Structure
  30. GC34071 Pamiparib (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
  31. 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
  32. 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
  33. 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
  34. GC68006 PARP1-IN-11 PARP1-IN-11  Chemical Structure
  35. 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
  36. 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
  37. 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
  38. 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
  39. GC68035 PARP10/15-IN-1 PARP10/15-IN-1  Chemical Structure
  40. 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
  41. 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
  42. GC69659 PARP11 inhibitor 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
  43. 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
  44. GC14251 Picolinamide poly (ADP-ribose) synthetase inhibitor Picolinamide  Chemical Structure
  45. 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
  46. 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
  47. 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
  48. GC13249 Rucaparib (free base) 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
  49. 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
  50. GC67962 Simmiparib Simmiparib  Chemical Structure
  51. 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
  52. GC37728 Talazoparib tosylate

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

    Talazoparib tosylate  Chemical Structure
  53. GC15041 Tankyrase Inhibitors (TNKS) 22 Tankyrase inhibitor Tankyrase Inhibitors (TNKS) 22  Chemical Structure
  54. GC11548 Tankyrase Inhibitors (TNKS) 49 Tankyrase inhibitor Tankyrase Inhibitors (TNKS) 49  Chemical Structure
  55. GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor Tankyrase-IN-2  Chemical Structure
  56. 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
  57. GC12781 XAV-939

    XAV-939 selectively inhibits β-catenin-mediated transcription.

    XAV-939  Chemical Structure

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