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Poly(ADP-ribose) glycohydrolase (PARG) inhibitors block the enzyme that removes poly(ADP-ribose) chains. After DNA damage, poly(ADP-ribose) polymerases (PARPs) build branched chains of this polymer on chromatin proteins to recruit repair factors. PARG hydrolyzes the bonds between the ribose units, which keeps the signal short-lived and releases bound proteins. The bovine PARG complementary DNA was isolated and characterized in 1997. Blocking PARG leaves poly(ADP-ribose) on chromatin and causes replication stress in some cancer cell lines. PDD 00017273 was reported in 2016 as a first-in-class cell-active PARG probe that inhibits DNA repair with pharmacology distinct from PARP inhibition. COH34, JA2131 and ethacridine are further inhibitors used to study poly(ADP-ribose) turnover.
Synonyms: NSC 36333
Ethacridine lactate is a topically applied anti-infective agent. Ethacridine lactate is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
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.
COH34 is a potent and selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG), with an IC50 of 0.37 nM. It binds to the catalytic domain of PARG (Kd = 0.547 μM), prolonging PARylation at sites of DNA damage and trapping DNA repair factors, thereby interfering with the DNA damage response.
JA2131 is a potent inhibitor of Poly(ADP-ribose) glycohydrolase (PARG) with an IC50 value of 0.4 μM. This compound effectively modulates DNA damage responses, leading to replication fork stalling and subsequent cancer cell death. JA2131 serves as a valuable tool for research in cancer biology and the elucidation of cellular repair mechanisms.
PARG-IN-4 is a potent and orally bioavailable inhibitor of poly(ADP-ribose) glycohydrolase (PARG), exhibiting an EC50 of 1.9 nM. This compound demonstrates favorable cell membrane permeability, making it suitable for in vivo studies. PARG-IN-4 effectively inhibits tumor growth in mouse models, and it is applicable in cancer research focused on the modulation of PARP-related pathways.
Ethacridine is a potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG), which plays a crucial role in the regulation of cellular responses to DNA damage. This compound has been shown to induce apoptosis in thyroid cancer cells, while also promoting differentiation in thyroid follicular cells. Its applications in cancer research and studies on cellular signaling pathways make it a valuable tool for understanding tumor biology and therapeutic interventions.
PDD00017272 is a potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with an EC50 of 4.8 nM. By inhibiting PARG activity, this compound promotes the accumulation of poly(ADP-ribose) (pADPr) on chromatin, thereby disrupting DNA damage repair and replication processes, leading to PARP1/2-dependent cytotoxicity. PDD00017272 is particularly valuable for research applications involving cancer models with DNA repair deficiencies, such as those characterized by BRCA mutations, and demonstrates enhanced efficacy in tumor cells exhibiting lower PARG expression.
PDD00017238 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), demonstrating EC50 values of 40 nM in biochemical assays and 55 nM in cellular assays. This compound effectively disrupts the enzymatic activity of PARG, leading to the accumulation of poly(ADP-ribose) chains and influencing DNA repair mechanisms. PDD00017238 is useful for studying the role of PARG in cellular processes, particularly in the context of DNA damage response and potential therapeutic strategies in oncology.
PDD00031705 is a benzimidazolone-based inhibitor targeting poly (ADP-ribose) glycohydrolase (PARG). This compound exhibits potential in regulating poly (ADP-ribose) metabolism, which plays a critical role in DNA damage repair and cell signaling. PDD00031705 is useful in research applications focused on understanding the physiological and pathological roles of PARG in cellular processes and its implications in cancer biology.
COH34 analog 1 is an oxidized derivative of the potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor, COH34. This compound specifically targets PARG, leading to the inhibition of poly(ADP-ribose) metabolism. Its role in PARG inhibition makes it a valuable tool for studying cellular processes involved in DNA repair, cellular stress responses, and other related pathways in chemical biology and therapeutic research.
PARG-IN-7 is a potent inhibitor of Poly ADP-ribose glycohydrolase (PARG), exhibiting an IC50 of less than 0.1 μM. This compound significantly reduces cell viability in HCC1806 cells with XRCC1 knockdown, demonstrating an IC50 of less than 1 μM. PARG-IN-7 is a valuable tool for cancer research, particularly in studies investigating the role of PARP-related pathways in tumor biology.
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PDD00031704 is an inhibitor of poly (ADP-ribose) glycohydrolase (PARG), demonstrated to have an IC50 value greater than 60 µM. It plays a crucial role in the regulation of ADP-ribosylation, impacting cellular processes such as DNA repair and apoptosis. This compound is valuable for research applications focused on cancer biology, cellular stress responses, and modulation of DNA damage pathways.
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FORX-428 is a selective and orally bioavailable inhibitor of Poly (ADP-ribose) glycohydrolase (PARG), which targets the catalytic domain of human PARG to effectively inhibit its enzymatic activity. By promoting the accumulation of PAR chains, FORX-428 activates DNA damage response pathways and replication stress responses. This compound demonstrates selective antiproliferative effects across a range of cancer cell lines, including those derived from breast, ovarian, and gastric cancers, making it a valuable tool for cancer research and therapeutic studies.
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