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.
PARP Isoform Specific Products
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PARP
(306)
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PARP1
(211)
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PARP2
(84)
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PARP3
(23)
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PARP4
(11)
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TNKS1/
PARP5A (41)View all products
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TNKS2/
PARP5B (38)View all products
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PARP7
(25)
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PARP10
(20)
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PARP14
(17)
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PARP15
(14)
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PARP12
(4)
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PARP16
(3)
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All Product Categories
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PARP Inhibitors
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PARP Agonists
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PARP Activators
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PARP Modulators
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PARP Inducers
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PARP Degraders
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PARP Substrate
(1)
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PARP Ligands
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PARP Related Products (699)
Related Products (699)
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Antibodies (11)
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PARP Isoform Comparison
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NSC666715
0 ImagesCat. No.: HY-120105CAS No.: 170747-33-8NSC666715 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.
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PARP-1/2-IN-2
0 ImagesCat. No.: HY-149398CAS No.: 3052304-23-8
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ROR1-IN-4
0 ImagesCat. No.: HY-175497ROR1-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).
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PARP1-IN-40
0 ImagesCat. No.: HY-174442PARP1-IN-40 is a highly selectively and orally active PARP1 inhibitor (IC50: 0.19 nM for PARP1, 26 nM for PARP2). PARP1-IN-40 kills tumor cells by inhibiting PARP1, leading to accumulation of DNA damage. PARP1-IN-40 has high antitumor activity against BRCA mutant MDA-MB-436 cells. PARP1-IN-40 can be used in combination with chemotherapy for cancer-related research.
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FLC-8
0 ImagesCat. No.: HY-182937CAS No.: 3100242-36-9FLC-8 is an orally active FLT3 inhibitor with IC50 values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia.
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ATWLPPRAANLLMAAS
0 ImagesCat. No.: HY-P10832CAS No.: 1228447-26-4ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..
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PARP1-IN-58
0 ImagesCat. No.: HY-187473PARP1-IN-58 is a ROS-responsive prodrug constructed based on a natural stilbene scaffold, and its active parent nucleus 24c acts as a selective PARP-1 inhibitor. PARP1-IN-58 only hydrolyzes to release the active parent compound in the high-ROS microenvironment of tumors; the active parent compound competitively binds to PARP-1 and blocks DNA single-strand damage repair, upregulates intracellular ROS levels, reduces mitochondrial membrane potential, and thereby induces cell cycle arrest and mitochondria-dependent apoptosis. PARP1-IN-58 exerts potent proliferation-inhibiting effects on BRCA-deficient breast cancer cells under simulated tumor oxidative stress conditions, and exhibits tumor growth inhibitory activity in breast cancer xenograft models. PARP1-IN-58 can be used in cancer-related research.
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NEURL1B-IN-1
0 ImagesCat. No.: HY-182008CAS No.: 3068938-30-4NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma.
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2'-Nitroflavone
0 ImagesCat. No.: HY-181068CAS No.: 53277-26-22'-Nitroflavone is a PARP1 inhibitor. 2'-Nitroflavone inhibits the proliferation, induces cell cycle arrest and apoptosis of triple-negative breast cancer cells. 2'-Nitroflavone also inhibits the migration of triple-negative breast cancer cells and endothelial cells. 2'-Nitroflavone exhibits antitumor activity and can be used in the research of tumors such as triple-negative breast cancer.
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PARP1/c-Met-IN-2
0 ImagesCat. No.: HY-178348PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP1/c-Met-IN-2 can be used for the study of Colon Cancer.
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PARP10-IN-1
0 ImagesCat. No.: HY-125217CAS No.: 2286261-72-9PARP10-IN-1 is a PARP10 inhibitor with an IC50 of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer.
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XZ8078
0 ImagesCat. No.: HY-184967XZ8078 is a potent, selective dual-target PROTAC degrader against PARP1 and IKZF3. In Capan-1 cells, XZ8078 exhibits a DC50 of 23.01 nM for PARP1 degradation and a DC50 of 23.20 nM for IKZF3 degradation. XZ8078 upregulates DNA damage markers in a concentration-dependent manner, induces cell cycle arrest, upregulates activated caspases and triggers apoptosis. XZ8078 inhibits tumor growth in both AZD5305-sensitive and AZD5305-resistant xenograft models. XZ8078 can be used for cancer-related research.
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HER4/HER2-IN-1
0 ImagesCat. No.: HY-178119HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer.
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MAHS-4
0 ImagesCat. No.: HY-187514MAHS-4 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR), with IC50 values of 1.918 μM and 83.53 μM, respectively. MAHS-4 inhibits thymidylate biosynthesis, reduces tetrahydrofolate pool maintenance, and interferes with extracellular matrix remodeling. MAHS-4 induces G2/M phase cell cycle arrest, activates endogenous caspase-dependent apoptosis, decreases MMP protein levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-4 is applicable for cancer-related research.
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IRS1
0 ImagesCat. No.: HY-P11902IRS1 is an integrin-targeted, ROS-responsive self-assembling peptide prodrug molecule with selective anti-cancer activity against integrin-overexpressing tumor cells. IRS1 contains an RGD motif for integrin binding, can covalently bind to DR4/DR5, and promotes DR4/DR5 aggregation. After oxidation by ROS, IRS1 undergoes a morphological transition from nanoparticles to nanofibers, exposes the pharmacophore of Chlorambucil (HY-13593), disrupts cell membrane integrity, activates the extrinsic apoptosis pathway, and can penetrate and inhibit the three-dimensional uveal melanoma spheroid model. IRS1 can be used for the research of uveal melanoma.
