2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Poly(ADP-ribose) Glycohydrolase (PARG)

Poly(ADP-ribose) Glycohydrolase (PARG)

Poly (ADP-ribose) glycohydrolase (PARG) is the primary hydrolase involved in the degradation of poly(ADP-ribose) (PAR). PARG possesses both endo-glycohydrolase and exo-glycohydrolase activity, preferentially performing the latter by binding to the two most distal ADP-ribose residues within the PAR chain. These different modes of catalysis produce free PAR and mono ADP-ribose moieties, respectively. The free mono ADP-ribose is then metabolized into AMP and ribose 5′ phosphate by ADP-ribose pyrophosphohydrolases such as the NUDIX family. AMP is utilized in ATP reformation and different metabolic and cell signaling pathways while ribose 5′ phosphate is a precursor to many biomolecules including DNA, RNA and ATP. Endo-glycohydrolase activity is considered to occur primarily during hyper-PARP activation, the resulting free PAR chains produced are then implicated in apoptosis acting as a death signal.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108360
    PDD 00017273
    		99.64%
    PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.
    PDD 00017273
  • HY-128760
    COH34
    		99.92%
    COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.
    COH34
  • HY-146248B
    TFMU-ADPr diammonium
    		Substrate 98.78%
    TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research.
    TFMU-ADPr diammonium
  • HY-133531
    PDD00017272
    		99.47%
    PDD00017272 is an inhibitor of poly(ADP-ribose) glycohydrolase (PARG) (EC50=4.8 nM) and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly(ADP-ribose) (pADPr), resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects (such as BRCA mutations) or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM (PARG cells), the tumor cells with lower PARG expression are more sensitive.
    PDD00017272
  • HY-P3017
    Endo-1,4-β-xylanase
    Endo-1,4-β-xylanase (Xylanase) is an arabinoxylan (AX) degrading enzyme and a glycoside hydrolase, is often used in biochemical studies. Endo-1,4-β-xylanase cleaves the β-xylosidic bond between two d-xylopyranosyl residues linked in β-(1,4).
    Endo-1,4-β-xylanase
  • HY-164717
    FORX-428
    		Inhibitor
    FORX-428 is a selective and orally active Poly (ADP-ribose) glycohydrolase (PARG) inhibitor. FORX-428 exhibits strong and reversible binding to the catalytic domain of human PARG, and thereby inhibits PARG´s enzymatic activity. FORX-428 leads to the excessive accumulation of PAR chains and activates DNA damage and replication stress responses. FORX-428 selectively inhibits the proliferation of various cancer cell lines, including breast, ovarian, and gastric cancer.
    FORX-428
  • HY-177420
    PDD00031704
    		Inhibitor
    PDD00031704 is a poly (ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of > 60 µM.
    PDD00031704
  • HY-177634B
    Gatuzosiran sodium scrambled negative control
    		Inhibitor
    Gatuzosiran sodium scrambled negative control is the sequence scrambled negative control of Gatuzosiran sodium.
    Gatuzosiran sodium scrambled negative control
  • HY-156881
    PARG-IN-4
    		Inhibitor 98.50%
    PARG-IN-4 (Formula (A)) is an orally available PARG inhibitor (EC50=1.9 nM) with cell membrane permeability. PARG-IN-4 can effectively inhibit tumor growth in mouse models. PARG-IN-4 can be used in cancer research.
    PARG-IN-4
  • HY-137924
    JA2131
    		Inhibitor 99.7%
    JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death.
    JA2131
  • HY-178208
    MDOLL-0286
    		Inhibitor 99.66%
    MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNA damage response. MDOLL-0286 can be used for the research of cancer .
    MDOLL-0286
  • HY-133530
    PDD00017238
    		98.71%
    PDD00017238 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with EC50 values of 40 nM and 55 nM in biochemical assay and cell POM, respectively.
    PDD00017238
  • HY-134354A
    pNP-ADPr disodium
    		98.08%
    pNP-ADPr disodium is a colorimetric substrate that used for the first continuous Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3) activity assays. pNP-ADPr disodium can be used for the research of poly(ADP-ribose)polymerase (PARP) enzymes.
    pNP-ADPr disodium
  • HY-135782A
    iso-ADP ribose TEA
    		99.97%
    iso-ADP ribose TEA is the small-molecule ligand for protein nucleic acid modification, comprising parts of two consecutive ADP-ribosyl units within the PAR chain. iso-ADP ribose TEA specifically binds WWE, FHA and OB-fold domains, enabling PAR-dependent functional responses like ubiquitylation and supporting DNA damage signaling and repair. iso-ADP ribose TEA can be used for cancer research.
    iso-ADP ribose TEA
  • HY-122041
    Ethacridine
    		Inhibitor 98.60%
    Ethacridine is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor and an activator of the transcriptional coactivator. Ethacridine induces thyroid cancer cells apoptosis and promotes differentiation in thyroid follicular cells.
    Ethacridine
  • HY-135846
    PDD00031705
    		99.47%
    PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG).
    PDD00031705
  • HY-158799
    Poly(ADP-ribose) Polymer/pADPr
    		Degrader
    Poly(ADP-ribose) Polymer/pADPr is a complex polymer of repeating ADP-ribose units, which is synthesized using poly(ADP-ribose) polymerase (PARP) in the presence of NAD+, cleaved from PARP, and subsequently purified.
    Poly(ADP-ribose) Polymer/pADPr
  • HY-135782
    iso-ADP ribose
    iso-ADP ribose is the small-molecule ligand for protein nucleic acid modification, comprising parts of two consecutive ADP-ribosyl units within the PAR chain. iso-ADP ribose specifically binds WWE, FHA and OB-fold domains, enabling PAR-dependent functional responses like ubiquitylation and supporting DNA damage signaling and repair. iso-ADP ribose can be used for cancer research.
    iso-ADP ribose
  • HY-115666
    COH34 analog 1
    		98.75%
    COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
    COH34 analog 1
  • HY-146248A
    TFMU-ADPr triethylamine
    		Substrate
    TFMU-ADPr triethylamine is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr triethylamine can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr triethylamine binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr triethylamine can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr triethylamine is also applicable to COVID-19-related research.
    TFMU-ADPr triethylamine
Cat. No. Product Name / Synonyms Application Reactivity