2. Signalwege
  3. Cell Cycle/DNA Damage
    Epigenetics
  4. PARP
  5. PARP Isoform

PARP

PARP-1 (poly(ADP-ribose) polymerase 1) is a nuclear ADP-ribosyl transferase that functions as an early sensor of DNA strand breaks and coordinates cellular responses to genomic damage through poly(ADP-ribosyl)ation-dependent signaling[1][2]. Mechanistically, PARP-1 participates in multiple DNA repair pathways, including base excision repair (BER), homologous recombination (HR), and non-homologous end joining (NHEJ), where it promotes chromatin remodeling and recruitment of repair factors to damaged DNA sites[1][2][3]. Through these activities, PARP-1 contributes to genome surveillance and maintenance of genomic stability, processes that are frequently disrupted during tumor development[1][2]. In cancer biology, dysregulated PARP-1 function has been associated with disease progression, and inhibition of PARP-mediated DNA repair can reduce tumor cell viability by exploiting defects in homologous recombination repair pathways[1][4]. Compared with the closely related isoform PARP-2, PARP-1 is the dominant mediator of single-strand break repair, whereas PARP-2 shares DNA repair functions but also displays distinct roles in biological processes including inflammation, metabolism, oxidative stress responses, and cancer progression[3][5]. This functional distinction is important for understanding isoform-specific biology and for designing selective therapeutic strategies[5]. For experimental and translational applications, PARP inhibitors have become widely used tools to interrogate DNA damage responses and to target tumors with DNA repair deficiencies, particularly those characterized by homologous recombination defects[1][4].

PARP Verwandte Produkte (299):

Art. -Nr. Produktname Wirkung Reinheit
  • HY-13688
    PJ34 hydrochloride
    		Inhibitor 99.81%
    PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively.
  • HY-N6818
    5,​7,​4'-​Trimethoxyflavone
    		Activator 99.65%
    5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress.
  • HY-137450
    Senaparib
    		Inhibitor 99.53%
    Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models.
  • HY-139534
    ARI-1
    		Activator 99.16%
    ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. ARI-1 upregulates cleaved-PARP and p-P38. ARI-1 induces Apoptosis. ARI-1 has anticancer activity against non-small cell lung cancer.
  • HY-N0660
    Jujuboside B
    		Activator 99.92%
    Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
  • HY-N1775
    3',4'-Dihydroxyacetophenone
    		Activator 99.92%
    3',4'-Dihydroxyacetophenone (3,4-DHAP) is a phenolic compound with oral bioavailability, possessing potent antioxidant, anti-inflammatory, anticancer and cardiovascular protective activities. 3',4'-Dihydroxyacetophenone inhibits mushroom Tyrosinase activity with an IC50 of 10 μM, thereby suppressing melanogenesis. 3',4'-Dihydroxyacetophenone inhibits platelet aggregation in platelet-rich plasma. 3',4'-Dihydroxyacetophenone reduces ROS levels in human umbilical vein endothelial cells treated with high glucose, upregulates the expression of Nrf2, HO-1 and PARP-1 in cells, and promotes the nuclear translocation of Nrf2. 3',4'-Dihydroxyacetophenone induces autophagy and apoptosis. 3',4'-Dihydroxyacetophenone inhibits seed germination/growth in most plants. 3',4'-Dihydroxyacetophenone can be used in the research of cancer, neurodegenerative diseases, non-alcoholic steatohepatitis, diabetes, obesity, skin pigmentation disorders, and cardiovascular and cerebrovascular diseases.
  • HY-75706
    N-Descyclopropanecarbaldehyde Olaparib
    		Inhibitor 99.46%
    N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 (HY-141481). N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
  • HY-108638
    NSC 146109 hydrochloride
    		Inhibitor 99.89%
    NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer.
  • HY-108631
    EB-47 dihydrochloride
    		Inhibitor 99.58%
    EB-47 dihydrochloride, 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. EB-47 mimics the substrate NAD+?and extends from the nicotinamide to the adenosine subsite.
  • HY-179078
    CT-179
    		Activator 99.79%
    CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC50 of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G2/M phase arrest and increases G0 population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma.
  • HY-120115
    PARPi-FL
    		Inhibitor 99.77%
    PARPi-FL (Olaparib-bodipy FL) is a small-molecule fluorescent inhibitor of PARP1 that can specifically bind to PARP1. PARPi-FL can be used as a fluorescent imaging agent for tumor detection, diagnosis, and surgical guidance.
  • HY-W015422
    1,5-Isoquinolinediol
    		Inhibitor 99.14%
    1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 μM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina.
  • HY-W042191
    Oxychlororaphine
    		Inducer 98.98%
    Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer.
  • HY-N8572
    3',4'-Dimethoxyflavone
    		Inhibitor 98.63%
    3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.
  • HY-N3677
    Dammarenediol II
    		Activator 99.81%
    Dammarenediol II is a ginsenoside precursor. Dammarenediol II reduces the activity of O-GlcNAc transferase (OGT) and downregulates the global O-GlcNAcylation level. Dammarenediol II inhibits the phosphorylation of Akt, mTOR and GSK3β. Dammarenediol II inhibits human carboxylesterase activity, VEGF-induced ROS production, stress fiber formation and vascular endothelial cadherin disruption. Dammarenediol II promotes cell apoptosis (apoptosis), increases the levels of cleaved PARP1 and p53, and inhibits retinal microvascular leakage. Dammarenediol II can be used in studies related to liver cancer and diabetic retinopathy.
  • HY-15044
    NU1025
    		Inhibitor 98.05%
    NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer agents. NU1025 has anti-cancer and neuroprotective activity.
  • HY-N2132
    Flavokawain B
    		99.99%
    Flavokawain B (Flavokavain B) is an orally active chalcone. Flavokawain B results in activation of caspase-9, -3 and -8, cleavage of PARP. Flavokawain B down-regulates Bcl-2 with concomitant increase in Bax level. Flavokawain B inhibits NF-κB, PI3K/Akt and MAPK signaling pathway. Flavokawain B exhibits Apoptotic effects. Flavokawain B inhibits MMP-9 and promotes ROS generation. Flavokawain B inhibits multiple tumors and inflammation.
  • HY-161430
    RTx-161
    		Inhibitor 98.0%
    RTx-161 is a DNA polymerase θ inhibitor with an IC50 of 4.1 nM. RTx-161 induces DNA damage, PARP cleavage, apoptosis, and selectively kills homologous recombination-deficient (HRD) cells. RTx-161 acts synergistically with PARP inhibitors to suppress PARP inhibitor resistance in cancer cells. RTx-161 can be used for the research of BRCAG12C mutant cancer and HR-deficient cancers.
  • HY-125911
    Gossypin
    		Inducer 98.29%
    Gossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.
  • HY-147291
    VPC-70063
    		Inhibitor 99.92%
    VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer.
Art. -Nr. Produktname / Synonyms Application Reactivity