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-141481
    DP-C-4
    Inhibitor 98.15%
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    DP-C-4
  • HY-164475
    PARP1-IN-29
    Inhibitor
    PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 value of 6.3 nM. PARP1-IN-29, after being labeled with [18F], can be used for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. PARP1-IN-29 is applicable in the fields of oncology and imaging research, particularly for detecting PARP-1 activity in cancer.
    PARP1-IN-29
  • HY-114324A
    rel-PROTAC PARP1 degrader
    Degrader 98.99%
    rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
    rel-PROTAC PARP1 degrader
  • HY-113432S
    Nudifloramide-d3
    Inhibitor ≥99.0%
    Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].
    Nudifloramide-d<sub>3</sub>
  • HY-146501
    PARP10/15-IN-2
    Inhibitor 99.00%
    PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis.
    PARP10/15-IN-2
  • HY-156332
    TNKS-2-IN-2
    Inhibitor 99.47%
    TNKS-2-IN-2 is a potent and selective inhibitor of TNKS2 with an IC50 of 22 nM.
    TNKS-2-IN-2
  • HY-157800
    Trilexium
    Activator 99.70%
    Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity.
    Trilexium
  • HY-105692
    DR2313
    Inhibitor 99.66%
    DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.
    DR2313
  • HY-155993
    YCH1899
    Inhibitor 99.39%
    YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.
    YCH1899
  • HY-147027
    PARP-1-IN-2
    Inhibitor 99.48%
    PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.
    PARP-1-IN-2
  • HY-147886
    PARP1-IN-11
    Inhibitor 98.58%
    PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC50 value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2.
    PARP1-IN-11
  • HY-153581
    ARTD3/PARP3-IN-1
    Inhibitor 99.64%
    ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3.
    ARTD3/PARP3-IN-1
  • HY-101020
    Picolinamide
    Inhibitor 99.97%
    Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
    Picolinamide
  • HY-116218C
    Amelparib hydrochloride
    Inhibitor 98.37%
    Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke.
    Amelparib hydrochloride
  • HY-102035
    PARP-2-IN-1
    Inhibitor 99.56%
    PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
    PARP-2-IN-1
  • HY-133124
    PARP/PI3K-IN-1
    Inhibitor 99.43%
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
    PARP/PI3K-IN-1
  • HY-163081
    PARP7-IN-17
    Inhibitor
    PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect.
    PARP7-IN-17
  • HY-23338
    TNKS-2-IN-1
    Inhibitor
    TNKS-2-IN-1 (Compound 13g) is a TNKS-2 inhibitor. TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM.
    TNKS-2-IN-1
  • HY-13540
    E7016
    Inhibitor 98.46%
    E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
    E7016
  • HY-148753
    PARP10-IN-2
    Inhibitor 98.02%
    PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively.
    PARP10-IN-2
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