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-118522
    TP-110
    Inhibitor
    TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.
    TP-110
  • HY-155766
    PARP1-IN-14
    Inhibitor
    PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cells with IC50 values below 0.3 nM.
    PARP1-IN-14
  • HY-178178
    PARP1-IN-46
    Inhibitor
    PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM. PARP1-IN-46 demonstrates remarkable anti-proliferative activity in both rat (C6) and human (U87MG) glioma cells. PARP1-IN-46 promotes PARP cleavage, triggers DNA damage, and increases ROS. PARP1-IN-46 effectively inhibits the migration, invasion and colony formation of glioma cells, and ultimately induces cell apoptosis. PARP1-IN-46 can be used to the study of glioma.
    PARP1-IN-46
  • HY-173259
    PARP7-IN-23
    Inhibitor
    PARP7-IN-23 (compound 56) is a potent PARP7 inhibitor with an EC50 of 0.915 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-23 has the potential for cancer research.
    PARP7-IN-23
  • HY-152198
    Tankyrase-IN-4
    Inhibitor
    Tankyrase-IN-4 is a tankyrase 1 (TNKS1) inhibitor with an IC50 value of 0.8 nM. Tankyrase-IN-4 can be used for the research of cancer.
    Tankyrase-IN-4
  • HY-158680
    PARP1-IN-21
    Inhibitor
    PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of < 10 nM.
    PARP1-IN-21
  • HY-173437
    CW-2
    Degrader
    CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)).
    CW-2
  • HY-P10285S
    d-KLA Peptide-d30
    d-KLA Peptide-d30 (D-(KLAKLAK)2-d30) is the deuterium labeled d-KLA Peptide (HY-P10285). d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects.
    d-KLA Peptide-d<sub>30</sub>
  • HY-RS10066
    PARP4 Human Pre-designed siRNA Set A
    Inhibitor

    PARP4 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PARP4 Human Pre-designed siRNA Set A
  • HY-175482
    PARP1-IN-43
    Inhibitor
    PARP1-IN-43 (Compound 5350) is a blood-brain barrier (BBB) permeable PARP1 inhibitor, with an IC50 of 5 nM. PARP1-IN-43 can be used for the study of homologous recombination (HR)-deficient central nerve system (CNS) cancers.
    PARP1-IN-43
  • HY-147514
    Anticancer agent 64
    Inhibitor
    Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
    Anticancer agent 64
  • HY-N15380
    4,4′-Secalonic acid D
    Inhibitor
    4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity.
    4,4′-Secalonic acid D
  • HY-174446
    PARP1-IN-39
    Inhibitor
    PARP1-IN-39 is an inhibitor of PARP1 with an IC50 of 0.22 nM. PARP1-IN-39 has an IC50 of 1.57 nM in human breast cancer cells. PARP1-IN-39 can be studied in breast, ovarian, pancreatic, and prostate cancers associated with DNA repair deficiencies, such as BRCA1/2 mutations.
    PARP1-IN-39
  • HY-N12999
    Stigmast-5-en-3-ol
    Agonist
    Stigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity.
    Stigmast-5-en-3-ol
  • HY-162643
    Antitumor agent-169
    Inhibitor
    Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics.
    Antitumor agent-169
  • HY-12601
    TNKS 22
    Inhibitor
    TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits TNKS1 and TNKS2 with IC50s of 0.1 and 4.1 nM, respectively.
    TNKS 22
  • HY-12602
    TNKS-IN-4
    Inhibitor
    TNKS-IN-4 (compound 49) is an orally active tankyrase (TNKS) inhibitor with IC50 values of 0.1 nM and 7.6nM for TNKS1 and TNKS2, respectively. TNKS-IN-4 can be used for study of APC-mutant colorectal cancer.
    TNKS-IN-4
  • HY-136778
    INH2BP
    Inhibitor
    INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases.
    INH2BP
  • HY-120339
    STK899704
    Inhibitor
    STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ​​ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.
    STK899704
  • HY-15050
    KCL-440
    Inhibitor
    KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1.
    KCL-440
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