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
- Cat.No. Product Name Information
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GC40468
1,5-Isoquinolinediol
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.
- GC62781 2-Methylquinazolin-4-ol 2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM.
- GC62805 4’-Methoxychalcone 4’-Methoxychalcone regulates adipocyte differentiation through PPARγ activation.
- 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.
- 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.
- GN10629 5,7-dihydroxychromone
- GC68161 5-AIQ
- GC45772 6(5H)-Phenanthridinone An inhibitor of PARP1 and 2
- GC12390 A-966492 A PARP1 and PARP2 inhibitor
- GC12422 ABT-888 (Veliparib)
- GC16318 AG-14361 A PARP1 inhibitor
- 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).
- GC16725 AZ6102 TNKS1/2 inhibitor
- GC46900 AZ9482 A PARP inhibitor
- GC17965 AZD2461 A PARP inhibitor
- GC62310 AZD5305 AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models.
- GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor
- GC14380 BGP-15 PARP inhibitor
- GC15932 BMN 673 A PARP inhibitor
- GC10920 BMN-673 8R,9S
- 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%.
- 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.
- 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.
- GC10690 BYK 204165 A selective inhibitor of PARP1
- GC14434 BYK 49187 Potent PARP-1/PARP-2 inhibitor
- GC47055 CAY10749 CAY10749 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. CAY10749 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
- GC47056 CAY10753 A TNKS2 inhibitor
- GN10040 Dehydrocorydaline
- GC12680 DR 2313 A PARP inhibitor
- 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.
- 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).
- GC12991 EB 47 A PARP1 and TNKS2 inhibitor
- GC50506 Fluorescein-NAD+ Fluorescent NAD+; substrate for ADP-ribosylation for use in PARP assays
- GC62121 Fluzoparib Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
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GC10456
Fucosterol
Fucosterol is a plant sterol found in algae
- GC13541 G007-LK tankyrase 1/2 inhibitor
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GC19542
GeA-69
GeA-69 is a selective, highly cell permeable allosteric inhibitor
- GC15353 Iniparib (BSI-201) A PARP1 inhibitor
- GC12496 INO-1001 A PARP inhibitor
- GC38385 INO-1001
- 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.
- GC65907 KSQ-4279 KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530).
- GC47693 m-Methoxybenzamide m-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. m-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum).
- GC13419 ME0328 PARP inhibitor,potent and selective
- GC62252 Mefuparib hydrochloride Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
- GC17802 MK-4827 An orally bioavailable PARP1/2 inhibitor
- 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.
- GC17052 MK-4827 Racemate selective inhibitor of PARP1/PARP2
- 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.
- GC16914 MN 64 tankyrase inhibitor
- GC62154 N-Descyclopropanecarbaldehyde Olaparib N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
- GC65202 Nesuparib Nesuparib is a potent inhibitor of PARP.
- 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.
- GC19264 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
- 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.
- GC17775 NU 1025 An inhibitor of PARP
- GC17555 NVP-TNKS656 TNKS2 inhibitor
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GC17580
Olaparib (AZD2281, Ku-0059436)
A PARP inhibitor
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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.
- GC67906 OM-153
- GN10114 Oroxin A
- GC45808 OUL35 An inhibitor of PARP10
- 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.
- 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.
- 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.
- GC65927 PARP-2-IN-1 PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
- GC68006 PARP1-IN-11
- GC62275 PARP1-IN-5 dihydrochloride PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
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GC69660
PARP1-IN-7
PARP1-IN-7 is an inhibitor of poly ADP-ribose polymerase-1 (PARP1), used as an anticancer agent.
- 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.
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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.
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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.
- GC68035 PARP10/15-IN-1
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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.
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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.
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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.
- GC39302 PARP14 inhibitor H10 PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
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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.
- GC14251 Picolinamide poly (ADP-ribose) synthetase inhibitor
- GC10995 PJ34 An inhibitor of poly (ADP-ribose) polymerases
- GC10145 PJ34 hydrochloride An inhibitor of poly (ADP-ribose) polymerases
- 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.
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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.
- GC62473 RBN012759 RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM.
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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
- 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.
- 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.
- GC15955 Rucaparib?(AG–014699,PF–01367338) phosphate A PARP1 inhibitor
- GC62105 Senaparib Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models.
- GC67962 Simmiparib
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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.
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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.
- GC15041 Tankyrase Inhibitors (TNKS) 22 Tankyrase inhibitor
- GC11548 Tankyrase Inhibitors (TNKS) 49 Tankyrase inhibitor
- GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor
- GC14509 UPF 1069 A selective PARP2 inhibitors
- GC17783 Veliparib dihydrochloride An orally bioavailable inhibitor of PARP1 and PARP2
- GC62129 Venadaparib Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research.
- GC33358 WD2000-012547 WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221.
- GC12781 XAV-939 XAV-939 selectively inhibits β-catenin-mediated transcription.