PARP
poly ADP ribose polymerase
PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. PARP1, PARP2, VPARP (PARP4), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity. Others include PARP3, PARP6, TIPARP (or PARP7), PARP8, PARP9, PARP10, PARP11, PARP12, PARP14, PARP15, and PARP16. PARP is found in the cell’s nucleus. The main role is to detect and signal single-strand DNA breaks (SSB) to the enzymatic machinery involved in the SSB repair.
PARP Isoform Specific Products
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PARP
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PARP1
(194)
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PARP2
(82)
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PARP3
(22)
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PARP4
(11)
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TNKS1/PARP5A
(40)
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TNKS2/PARP5B
(37)
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PARP7
(24)
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PARP10
(20)
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PARP14
(17)
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PARP15
(14)
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PARP12
(4)
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PARP16
(3)
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All Product Categories
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PARP Inhibitors
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PARP Agonists
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PARP Activators
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PARP Modulators
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PARP Inducers
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PARP Degraders
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PARP Substrate
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PARP Ligands
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PARP Related Products (653)
Related Products (653)
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Antibodies (11)
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PARP Isoform Comparison
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Tambiciclib
0 ImagesSynonyms: GFH009; JSH-009; SLS009Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research.
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Fluzoparib
0 ImagesSynonyms: SHR3162; FuzuloparibFluzoparib (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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Fucosterol
0 ImagesFucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.
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Pamiparib
0 ImagesSynonyms: BGB-290Pamiparib (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 has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.
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Taurodeoxycholic acid
0 ImagesTaurodeoxycholate sodium salt is a bile salt-related anionic detergent. Taurodeoxycholic acid is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholic acid is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholic acid (TDCA) exhibits anti-inflammatory and neuroprotective effects.
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RBN012759
0 ImagesRBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.
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Dehydrocorydaline
0 ImagesSynonyms: 13-MethylpalmatineDehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
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Niraparib hydrochloride
0 ImagesSynonyms: MK-4827 hydrochloride
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WIKI4
0 ImagesWIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
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Daphnetin
0 ImagesDaphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
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Purine
0 ImagesPurine is an endogenous metabolite. Purine bases are the building blocks of the nucleic acids. Purine inhibits the activation of PARP. Purine protects against oxidant-induced cell injury. Purine can be used in the research of cancer and nervous system diseases.
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Sweroside
0 ImagesSweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields.
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JQAD1
0 ImagesJQAD1 is a EP300 PROTAC degrader. JQAD1 selectively targets EP300 and induces its degradation via the CRBN-dependent proteasomal pathway. JQAD1 reduces the levels of H3K27ac and the expression of MYCN. JQAD1 induces apoptosis (apoptosis) and inhibits cancer cell growth. JQAD1 exerts anti-neuroblastoma effects in vivo in a CRBN-dependent manner. JQAD1 can be used for the research of neuroblastoma.
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Rucaparib phosphate
0 ImagesSynonyms: AG-014699 phosphate; PF-01367338 phosphateRucaparib (AG014699) phosphate 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 phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research.
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Basroparib
0 ImagesSynonyms: STP1002Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors.
