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-158138
    TOPOI/PARP-1-IN-1
    Inhibitor
    TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%.
    TOPOI/PARP-1-IN-1
  • HY-145328
    PARP-1/2-IN-1
    PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.
    PARP-1/2-IN-1
  • HY-172971
    ARCher-142
    Inhibitor
    ARCher-142 (compound S8) is a potent tankyrase inhibitor. ARCher-142 selectively binds to ARC4 with potency of 8 µM.
    ARCher-142
  • HY-N0576R
    Solanesol (Standard)
    Inhibitor
    Solanesol (Standard) is the analytical standard of Solanesol (HY-N0576). This product is intended for research and analytical applications. Solanesol is an orally active aliphatic terpene alcohol. Solanesol is mainly found in tobacco and other Solanaceae plants. Solanesol induces HO-1 and Hsp70 expression, activates p38 and Akt signaling pathways, and inhibits Apoptosis (reduces caspase-3 and PARP cleavage). Solanesol has antioxidant, anti-inflammatory, and neuroprotective activities. Solanesol can be used in the research of Huntington's disease, alcoholic liver disease, chronic inflammatory pain, anxiety, Alzheimer's disease, and bipolar disorder.
    Solanesol (Standard)
  • HY-168722
    PROTAC PARP1 degrader-3
    Degrader
    PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for PARP1 with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC50 of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 (HY-13704) in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095); Pink: Ligand for target protein (HY-10619); Black: Linker (HY-16872))
    PROTAC PARP1 degrader-3
  • HY-170972
    PARP1/NAMPT-IN-2
    Inhibitor
    PARP1/NAMPT-IN-2 (Compound 13j) is a dual PARP/NAMPT inhibitor with IC50 values of 0.8 nM and 18 nM for PARP1 and NAMPT, respectively. PARP1/NAMPT-IN-2 can inhibit the proliferation, migration and induce apoptosis of breast cancer cells. PARP1/NAMPT-IN-2 can be used for the research of triple-negative breast cancer.
    PARP1/NAMPT-IN-2
  • HY-105303
    CEP-9722
    Inhibitor
    CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects.
    CEP-9722
  • HY-161607
    PARP7-IN-21
    Inhibitor
    PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC50 of < 10 nM.
    PARP7-IN-21
  • HY-N0281R
    Daphnetin (Standard)
    Inducer
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin (Standard)
  • HY-182044
    MRTX849-amide-C4-(o)-carborane
    Activator
    MRTX849-amide-C4-(o)-carborane is a KRASG12C inhibitor with mutation selectivity for cells expressing KRASG12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRASG12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRASG12C-positive cancers.
    MRTX849-amide-C4-(o)-carborane
  • HY-170942
    CDK9/PARP-IN-1
    Inhibitor
    CDK9/PARP-IN-1 (compound 37) is a CDK9/PARP inhibitor. CDK9/PARP-IN-1 inhibits CDK9 and PARP1 with IC50s of 118 and 107 nM, respectively. CDK9/PARP-IN-1 exhibits broad-spectrum antiproliferative effects across multiple cancer cell lines.
    CDK9/PARP-IN-1
  • HY-181723
    Anticancer agent 304
    Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer.
    Anticancer agent 304
  • HY-170967
    IPH10
    IPH10 is an anti-cancer agent that exhibits a strong anti-tumor effect in vivo without hepatic and renal toxicity. IPH10 can significantly increase the content of ROS, decrease the mitochondrial membrane potential, and induce apoptosis in tumor cells.
    IPH10
  • HY-182957
    MNK/PIM-IN-2
    Modulator
    MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC50 of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia.
    MNK/PIM-IN-2
  • HY-180926
    PARP10-IN-4
    Inhibitor
    PARP10-IN-4 (compound 12Z) is a potent PARP10 inhibitor with a pIC50 of 7.95. also shows inhibitory activity against TNKS1, TNKS2, and PARP11 with pIC50 values of 6.95, 7.03, and 7.01, respectively.
    PARP10-IN-4
  • HY-120105
    NSC666715
    Activator
    NSC666715 is a DNA polymerase β (Pol-β) inhibitor. NSC666715 directly and specifically interacts with Pol-β, interferes with its binding to damaged DNA, blocks its dRP lyase activity, and inhibits Pol-β-mediated SN- and LP-BER. NSC666715 induces AP site accumulation and S-phase cell cycle arrest, and triggers senescence and apoptosis (apoptosis) via the p53/p21 pathway in colorectal cancer cells. NSC666715 enhances TMZ (HY-17364)-induced DNA damage, senescence and apoptosis, and potentiates the cytotoxicity of TMZ. NSC666715 inhibits tumor growth in colon cancer xenograft models. NSC666715 can be used in research related to colorectal cancer.
    NSC666715
  • HY-155038
    Antitumor agent-104
    Inhibitor
    Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12.
    Antitumor agent-104
  • HY-149398
    PARP-1/2-IN-2
    Inhibitor
    PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor.
    PARP-1/2-IN-2
  • HY-175497
    ROR1-IN-4
    Activator
    ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC).
    ROR1-IN-4
  • HY-163461
    4F-DDC
    Inhibitor
    4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts.
    4F-DDC
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