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PARP-1/2-IN-1

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24

Inhibitors & Agonists

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Natural
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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12418
    Stenoparib
    2 Publications Verification

    E7449; 2X-121

    		 PARP Cancer
    Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
    Stenoparib
  • HY-139156
    SK-575
    5 Publications Verification

    		 PROTACs PARP Cancer
    SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .
    SK-575
  • HY-123851
    MSC2504877

    M2912

    		 PARP Cancer
    MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity .
    MSC2504877
  • HY-N1775
    3',4'-Dihydroxyacetophenone

    3,4-DHAP

    		 Tyrosinase Reactive Oxygen Species (ROS) Keap1-Nrf2 PARP Autophagy Apoptosis Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    3',4'-Dihydroxyacetophenone (3,4-DHAP) is a phenolic compound with oral bioavailability, possessing potent antioxidant, anti-inflammatory, anticancer and cardiovascular protective activities. 3',4'-Dihydroxyacetophenone inhibits mushroom Tyrosinase activity with an IC50 of 10 μM, thereby suppressing melanogenesis . 3',4'-Dihydroxyacetophenone inhibits platelet aggregation in platelet-rich plasma. 3',4'-Dihydroxyacetophenone reduces ROS levels in human umbilical vein endothelial cells treated with high glucose, upregulates the expression of Nrf2, HO-1 and PARP-1 in cells, and promotes the nuclear translocation of Nrf2 . 3',4'-Dihydroxyacetophenone induces autophagy and apoptosis. 3',4'-Dihydroxyacetophenone inhibits seed germination/growth in most plants. 3',4'-Dihydroxyacetophenone can be used in the research of cancer, neurodegenerative diseases, non-alcoholic steatohepatitis, diabetes, obesity, skin pigmentation disorders, and cardiovascular and cerebrovascular diseases .
    3',4'-Dihydroxyacetophenone
  • HY-146336
    PARP1/2/TNKS1/2-IN-1

    		PARP Apoptosis Cancer
    PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis .
    PARP1/2/TNKS1/2-IN-1
  • HY-179406
    PARP1-IN-49

    		PARP DNA/RNA Synthesis Reactive Oxygen Species (ROS) Apoptosis Cancer
    PARP1-IN-49 is a selective PARP1 inhibitor with an IC50 of 23.56 nM and a Kd of 17.78 nM. PARP1-IN-49 shows a selectivity for PARP1 over PARP2. PARP1-IN-49 leads to the induction of DNA damage, cell cycle arrest, and apoptosis. PARP1-IN-49 also increases intracellular ROS levels and inhibits cell migration. PARP1-IN-49 can be used for the research of breast cancer and ovarian cancer .
    PARP1-IN-49
  • HY-179386
    PARP1/EZH2-IN-1

    		PARP Histone Methyltransferase Apoptosis Pyroptosis Necroptosis Reactive Oxygen Species (ROS) PANoptosis Cancer
    PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research .
    PARP1/EZH2-IN-1
  • HY-105253
    PARP-2/1-IN-2

    		PARP Neurological Disease
    PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity [1].
    PARP-2/1-IN-2
  • HY-178100
    PARP1-IN-45

    		PARP BCRP Cancer
    PARP1-IN-45 (Compound 15) is a PARP1 inhibitor with an IC50 of 17  nM. PARP1-IN-45 effectively stimulates ATPase activity of ABCG2. PARP1-IN-45 can be used for cancers like ovarian cancer research .
    PARP1-IN-45
  • HY-149398
    PARP-1/2-IN-2

    		Apoptosis PARP CDK Cancer
    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-157165
    Tubulin/PARP-IN-1

    		Microtubule/Tubulin PARP Cancer
    Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
    Tubulin/PARP-IN-1
  • HY-145328
    PARP-1/2-IN-1

    		PARP Others
    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-174442
    PARP1-IN-40

    		PARP Cancer
    PARP1-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 .
    PARP1-IN-40
  • HY-174446
    PARP1-IN-39

    		PARP Cancer
    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-168657
    PARP1/2-IN-4

    		PARP Others
    PARP1/2-IN-4 (compound 3) is a PARP1/2 inhibitor .
    PARP1/2-IN-4
  • HY-169299
    TOPOI/PARP-1-IN-2

    		PARP Topoisomerase Apoptosis Cancer
    TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines .
    TOPOI/PARP-1-IN-2
  • HY-183765
    PARP1/PKM2-IN-1

    		PARP Pyruvate Kinase Cancer
    PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma .
    PARP1/PKM2-IN-1
  • HY-161868
    DLC-50

    		PARP HDAC Apoptosis Cancer
    DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
    DLC-50
  • HY-162802
    PI3K/AKT-IN-4

    		Apoptosis PI3K Akt PARP CDK Cancer
    PI3K/AKT-IN-4 (compound 3) is a diterpenoid that can be isolated from the roots and rhizomes of Salvia castanea Dielsf. PI3K/AKT-IN-4 has antitumor activity, inhibiting cell viability and proliferation (IC50=4.72 μM) and promoting apoptosis by blocking the G0/G1 phase of the Hep3B cell cycle, inducing mitochondrial dysfunction and oxidative stress. In addition, PI3K/AKT-IN-4 inhibits hepatocellular carcinoma by inhibiting the PI3K-Akt signaling pathway and binding to PARP1 and CDK2 targets .
    PI3K/AKT-IN-4
  • HY-181928
    PARP1/c-Met-IN-3

    		c-Met/HGFR PARP Apoptosis Cancer
    PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer .
    PARP1/c-Met-IN-3
  • HY-181460
    PARP1 degrader-2

    		HyT PARP Cancer
    PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .
    PARP1 degrader-2
  • HY-183317
    IDO1-IN-34

    		Indoleamine 2,3-Dioxygenase (IDO) Interleukin Related Apoptosis Caspase PARP Cancer
    IDO1-IN-34 is a selective IDO1 inhibitor with an IC50 of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia .
    IDO1-IN-34
  • HY-181746
    Bcl-2/Mcl-1-IN-5

    		Bcl-2 Family Apoptosis Caspase PARP Cancer
    Bcl-2/Mcl-1-IN-5 (Compound S6) is a Bcl-2 and Mcl-1 inhibitor. Bcl-2/Mcl-1-IN-5 promotes Apoptosis, downregulates anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane potential depolarization, and activates the Caspase-dependent apoptotic cascade, as evidenced by Caspase-3 activation and PARP1 cleavage. Bcl-2/Mcl-1-IN-5 has anti-hepatocellular carcinoma activity .
    Bcl-2/Mcl-1-IN-5
  • HY-183013
    PROTAC PARP2 degrader-1

    		PROTACs PARP Apoptosis Cancer
    PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .
    PROTAC PARP2 degrader-1

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