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PARP

Poly (ADP-ribose) polymerase (PARP) is a family of proteins involved in a number of cellular processes such as DNA repair, genomic stability, and programmed cell death.

  • Niraparib
    T32311038915-60-4
    Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.
    • $55
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  • Olaparib
    T3015763113-22-0
    Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.
    • $31
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  • RBN012759
    T224142360851-29-0
    RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.
    • $107
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  • 3-Aminobenzamide
    T63293544-24-9
    3-Aminobenzamide (PARP-IN-1) is an effective inhibitor of PARP (IC50<50 nM in CHO cells) and a mediator of oxidant-induced myocyte dysfunction during reperfusion.
    • $37
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  • EB-47
    T11143366454-36-6In house
    EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite.EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM.
    • $62
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  • 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
    TN5263569-83-5
    1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.
    • $36
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  • MK-4827 Racemate
    T229881038915-75-1
    MK-4827 Racemate (Niraparib Racemate) is a selective PARP1 and PARP2 inhibitor with IC50s of 3.8 nM and 2.1 nM, respectively, over 330-fold selectivity for PARP3, V-PARP and Tank1.
    • $45
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  • PARP-2-IN-3
    T730272915650-86-9In house
    PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.CAS 번호128-52-56-8
    • $350 TargetMol
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  • ARTD10/PARP10-IN-1
    T725531708103-76-7
    ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.
    • $350
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  • PARP1/2/TNKS1/2-IN-1
    T724372243453-32-7In house
    PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has potential anti-tumor activity and induces apoptosis.
    • $70
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  • VPC-70063
    T6001913571-44-3
    VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max/UBE2C downstream pathway inhibition of 94%. VPC-70063 can be used for studies about anticancer.
    • $58
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  • AG14361
    T6339328543-09-5In house
    AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).
    • $47
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  • Veliparib
    T2591912444-00-9
    Veliparib (ABT-888) (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy.
    • $52
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  • XAV-939
    T1878284028-89-3
    XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.
    • $48
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  • PJ34
    T6197344458-19-1
    PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
    • $48
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  • AZD-2461
    T24841174043-16-3
    AZD2461 is a novel PARP inhibitor.
    • $32
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  • Talazoparib
    T62531207456-01-6
    Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).
    • $35
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  • PI-1840
    T69411401223-22-0
    PI-1840(IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
    • $54
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  • Verbascoside
    T337561276-17-3
    Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
    • $58
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  • PARP-1-IN-3
    T781572976342-33-1
    PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.
    • $39
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  • SK-575
    T695962523016-96-6
    SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.SK-575 effectively inhibits the growth of cancer cells harboring BRCA1/2 mutations and selectively induces PARP1 degradation in cancer cells.
    • $107
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  • Excisanin A
    TN404678536-37-5
    ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).
    • $980
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  • Ivangustin
    TN434014164-59-1
    Ivangustin, a sesquiterpene lactone derived from the medicinal plant Inula britannica, exhibits significant cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines.
    • $193
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  • Kuguaglycoside C
    TN18371041631-93-9
    Kuguaglycoside C induces caspase-independent cell death, and is involved, at least in part, in the mechanism underlying cell necroptosis.
    • $790
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  • PARP1-IN-17
    T81543
    PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis. It exhibits robust anti-proliferative activity [1].
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  • Ru3
    T81249
    Ru3 is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor that prompts apoptosis in MCF-7 cells through various mechanisms, including DNA damage induction, inhibition of DNA repair, alteration of cell cycle distribution, reduction of mitochondrial membrane potential, and elevation of intracellular reactive oxygen species (ROS) levels [1].
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  • PARP7-IN-16
    T815412435657-10-4
    PARP7-IN-16 (compound 36) is a potent, selective, and orally active PARP-1/2/7 inhibitor, exhibiting IC50 values of 0.94, 0.87, and 0.21 nM , respectively. It has potential applications in breast and prostate cancer research [1].
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  • Sageone
    TN4932142546-15-4
    Sageone represents a promising anticancer agent against gastric cancer that warrants further study, it synergizes with cisplatin cytotoxicity in SNU-1 human gastric cancer cells.Sageone also shows antiviral activity.
    • $3,209
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  • Euchrestaflavanone B
    TN402887402-91-3
    Euchrestaflavanone B shows antibacterial activity against Gram positive bacteria, Staphylococcus aureus, Bacillus subtilis and Bacillus cereus. Euchrestaflavanone B may function by inhibiting oncogenic disease, at least in part, through the inhibition of
    • $2,028
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  • IVHD-valtrate
    TN434128325-56-6
    VHD-valtrate has anticancer effects against human ovarian cancer cells in vitro and in vivo, it is a potential therapeutic agent for ovarian cancer, providing a basis for development of the compound as a novel chemotherapeutic agent.
    • $2,998
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  • Cedrusin
    TN361975775-36-9
    Cedrusin shows a cytotoxic effect on A375 and HeLa cells.
    • $1,498
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  • Hellebrigenin
    TN1728465-90-7
    Hellebrigenin has anti-hepatoma activities, it induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Hellebrigenin exhibites moderate to strong activity against human HL-60, SF-295, MDA-MB-435, and HCT-8 cancer cell strains without hemolysis of mouse erythrocytes.
    • $898
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  • Cearoin
    TN361452811-37-7
    Cearoin has anti-inflammatory, and antiallergic activities, it can markedly inhibit inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS mRNA and LPS-induced mRNA expression of TNFα and CCL2. Cearoin induces aut
    • $524
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  • Boehmenan
    TN352557296-22-7
    (±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell
    • $276
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  • PARP1-IN-16
    T81544
    PARP1-IN-16 (compound 12a) serves as a potent PARP1 inhibitor, exhibiting an IC50 value of 1.89 nM. It possesses the capability to halt the cell cycle at the S phase and stimulate apoptosis in HCT-116 cells [1].
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  • TNKS-2-IN-1
    T776754765-59-7
    TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.
    • $30
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  • Effusanin E
    TN392276470-15-0
    Effusanin E shows antibacterial and anti-cancer activities, it significantly inhibits cell proliferation and induces apoptosis in NPC cells by suppressing p50/p65 proteins to down-regulate COX-2 expression .
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  • Dehydrocavidine
    TN113983218-34-2
    Dehydrocavidine (Dehydrocorydaline) has antitumor activity, it inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.
    • $207
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  • WAY-620473
    T67945743451-55-0
    WAY-620473 is a potent PARP-1 inhibitor with antitumor activity and alters eukaryotic lifespan.
    • $39
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  • Neogrifolin
    TN463723665-96-5
    Neogrifolin is a potential candidate for osteosarcoma, it can induce concentration- and time-dependent suppression of proliferation and induce apoptosis in U2OS and MG63 osteosarcoma cell lines; it exhibits inhibitory activity against nitric oxide (NO) production stimulated by lipopolysaccharide (LPS) in RAW 264.7 cells with the IC50value of 23.3 microM. Neogrifolin possesses antimicrobial activities against Bacillus cereus and Enterococcus faecalis, the MIC values of 20 and 0.5 microg/mL, respectively.
    • $1,790
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  • G244-LM
    T89641563007-08-8
    G244-LM is a potent and specific inhibitor of tankyrase 1/2. G244-LM inhibits Wnt signaling.
    • $44
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  • DR2313
    T22749284028-90-6
    DR2313 is a competitive inhibitor of poly(ADP-ribose) polymerase (IC50: 0.20 and 0.24 μM for PARP-1 and PARP-2 respectively). It also has neuroprotective.
    • $50
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  • Ganoderic acid DM
    TN1663173075-45-1
    Ganoderic acid DM is an antiandrogenic osteoclastogenesis inhibitor, it especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1), this suppression leads to the inhibition of dendritic cell-specific transmembrane pr
    • $275
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  • GeA-69
    T53992143475-98-1
    GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
    • $59
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  • PARP-1-IN-4
    T78182684234-56-8
    PARP-1-IN-4 is a potent PARP-1 inhibitor with potential see anti-tumor activity, and inhibition of PARP-1 may be used in cancer development.
    • $39
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  • PARP7-IN-15
    T815422819998-97-3
    PARP7-IN-15 (Compound 18) is a potent PARP7 inhibitor exhibiting an IC50 of 0.56 nM and demonstrates antitumor activity [1].
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  • 4'-Methoxychalcone
    T7443959-23-9
    4'-Methoxychalcone with a variety of pharmacological activities, such as anti-tumor and anti-inflammatory activities.
    • $39
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  • 5-AIQ
    T5004493117-08-9
    5-aminoisoquinolin-1(2H)-one is the inhibitor of calf thymus PARP1.
    • $47
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  • PARP/HDAC-IN-1
    T85321
    PARP HDAC-IN-1 is a selective PARP and HDAC inhibitor with potential anticancer activity, inhibits PARP1, PARP2 and HDAC1, and may be used in the study of pancreatic cancer.
    • $195
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  • PARP-1/2-IN-2
    T78787
    PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC 50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair and inducing cell cycle arrest and apoptosis. This compound also hampers the proliferation of TNBC cells and the growth of TNBC xenograft tumors [1].
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