1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Epigenetics
  3. PARP

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130646
    iVeliparib-AP6
    Degrader
    iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC50s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC50s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism.
    iVeliparib-AP6
  • HY-176713
    KWZY-11
    Inhibitor
    KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells.
    KWZY-11
  • HY-12577
    TNKS1/2-IN-1
    Inhibitor 99.24%
    TNKS1/2-IN-1 (Example 4) is a TNKS1 and TNKS2 inhibitor, with pIC50 values of 8.2 or 7.3 against TNKS1, and 7.1 or 7.7 against TNKS2. TNKS1/2-IN-1 inhibits the enzymatic activities of TNKS1 and TNKS2. TNKS1/2-IN-1 is applicable for cancer research.
    TNKS1/2-IN-1
  • HY-153590
    PARP-1-IN-4
    Inhibitor 99.74%
    PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma.
    PARP-1-IN-4
  • HY-156432
    ALK-IN-26
    Activator 99.87%
    ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies.
    ALK-IN-26
  • HY-153581
    ARTD3/PARP3-IN-1
    Inhibitor 99.64%
    ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3.
    ARTD3/PARP3-IN-1
  • HY-W156961
    LS-75
    Inhibitor 99.31%
    LS-75 is a PARP-1 inhibitor with blood-brain permeability and IC50 value of 18 μM. LS-75 has neuroprotective activity.
    LS-75
  • HY-123232
    KU-0058684
    Inhibitor
    KU-0058684 is a potent PARP inhibitor, with an IC50 of 3.2 nM for PARP-1. KU-0058684 significantly reduces DNA double strand break (DSB) repair.
    KU-0058684
  • HY-10617C
    Rucaparib tartrate
    Inhibitor
    Rucaparib (AG014699) tartrate 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 tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research.
    Rucaparib tartrate
  • HY-102003A
    Rucaparib camsylate
    Inhibitor
    Rucaparib (AG014699) camsylate 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
  • HY-N6818R
    5,​7,​4'-​Trimethoxyflavone (Standard)
    Activator
    5,​7,​4'-​Trimethoxyflavone (Standard) is the analytical standard of 5,​7,​4'-​Trimethoxyflavone. This product is intended for research and analytical applications. 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.
    5,​7,​4'-​Trimethoxyflavone (Standard)
  • HY-132297
    PARP1-IN-5
    Inhibitor
    PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
    PARP1-IN-5
  • HY-13559
    Atiprimod
    Activator
    Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML).
    Atiprimod
  • HY-137457A
    Venadaparib hydrochloride
    Inhibitor
    Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research.
    Venadaparib hydrochloride
  • HY-128344
    BR102375
    Agonist
    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
  • HY-178749
    MS6076
    MS6076 is a mitochondrial protease ClpP agonist. MS6076 specifically activates the ClpP protease in the mitochondrial matrix, significantly disrupting mitochondrial Electron Transport Chain (ETC) function by accelerating the degradation of unfolded proteins. MS6076 exhibits potent cytotoxicity against a variety of cancer cell lines. MS6076 induces cell apoptosis, increasing cleavage of caspase 3 and PARP. MS6076 can be used for the research of breast cancer.
    MS6076
  • HY-10617D
    Rucaparib acetate
    Inhibitor
    Rucaparib (AG014699) acetate 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 acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research.
    Rucaparib acetate
  • HY-145584A
    Nesuparib hydrochloride
    Inhibitor
    Nesuparib (JPI-547) hydrochloride is the orally active inhibitor for PARP 1/2 and Tankyrase 1/2 that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC50s of 5, 1 and 2 nM, respectively. Nesuparib hydrochloride exhibits antitumor activity and can be used in research of advanced solid tumor.
    Nesuparib hydrochloride
  • HY-10617B
    Rucaparib hydrochloride
    Inhibitor
    Rucaparib (AG014699) hydrochloride 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 hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research.
    Rucaparib hydrochloride
  • HY-113432S1
    Nudifloramide-d6
    Inhibitor
    Nudifloramide-d6 (2PY-d6) is deuterium-labeled Nudifloramide (HY-113432).
    Nudifloramide-d<sub>6</sub>
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