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

PARP

poly ADP ribose polymerase

PARP

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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:

PARP Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-181999
    PC8
    		Inhibitor
    PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.
    PC8
  • HY-183143
    Lss-11
    		Activator
    Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer.
    Lss-11
  • 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-181967
    PROTAC PARP1 degrader-5
    		Degrader
    PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma.
    PROTAC PARP1 degrader-5
  • 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
  • HY-D1188
    PARP7-probe-1
    PARP7-probe-1 is a chemiluminescent labeled PARP7 probe. PARP7-probe-1 is a biotinylated probe binding to the PARP7 active site. PARP7-probe-1 can be used for the research of PARP7 function.
    PARP7-probe-1
  • HY-151624
    PARP-2-IN-2
    		Inhibitor
    PARP-2-IN-2 (compound 27) is a PARP 2 inhibitor with an IC50 value of 0.057 μM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer.
    PARP-2-IN-2
  • HY-178099
    Apoptosis inducer 45
    		Inhibitor
    Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer.
    Apoptosis inducer 45
  • HY-181027
    TIPARP-IN-1
    		Inhibitor
    TIPARP-IN-1 (Compound 15) is a selective PARP7 (TIPARP) (2,3,7,8-Tetrachlorodiben-zo-p-dioxin(TCDD)-inducible PARP) inhibitor with an IC50 of 2.15 nM. TIPARP-IN-1 can restore IFN signaling pathway in tumors by inhibiting TIPARP. TIPARP-IN-1 selectively activates the anti-tumor immune response in the tumor microenvironment and avoids the production of systemic cytokines. TIPARP-IN-1 can be used for research of head and neck squamous cell carcinoma.
    TIPARP-IN-1
  • HY-15276
    4-Aminonaphthalimide
    		Inhibitor
    4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells.
    4-Aminonaphthalimide
  • HY-162349
    PARP7/HDACs-IN-1
    		Inhibitor
    PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6). br/.
    PARP7/HDACs-IN-1
  • HY-179685
    PARP1-IN-51
    		Inhibitor
    PARP1-IN-51 (P55 the second compound in the fifth row) is a PARP1 inhibitor. PARP1-IN-51 can be used for the research of cancer, such as breast cancer.
    PARP1-IN-51
  • HY-171543
    PARP1-IN-37
    		Inhibitor
    PARP1-IN-37 (Compound 8) is an orally active and selective poly(ADP-ribose) polymerase 1 and 2 (PARP1/2) inhibitor with an IC50 value of 24 nM for PARP1. PARP1-IN-37 inhibits PARP activity in cells with an EC50 value of 3.7 μM. PARP1-IN-37 is promising for research of BRCA-mutated tumors, such as breast and ovarian cancers.
    PARP1-IN-37
  • HY-16483
    Telapristone acetate
    		Inhibitor
    Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research.
    Telapristone acetate
  • HY-182269
    Cathepsin-IN-5
    Cathepsin-IN-5 is a cathepsin inhibitor with IC50 values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma.
    Cathepsin-IN-5
  • HY-152197
    Tankyrase-IN-3
    		Inhibitor
    Tankyrase-IN-3 is a tankyrase 1 (TNKS1) inhibitor with an IC50 value of 22 nM. Tankyrase-IN-3 can be used for the research of cancer.
    Tankyrase-IN-3
Cat. No. Product Name / Synonyms Application Reactivity
PARP Isoform Comparison

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