adp-ribose

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum and facilitates extracellular influx via TRPM2 channels [1][2][3].

TH5427 is a lead NUDT5 inhibitor(MG assay IC50 = 29 nM).

Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release and extracellular influx via the opening of TRPM2 channels.

ADP-ribose/PARP-IN-1 (Compound Ex.16) is a conjugated compound composed of a disease-targeting segment, a PARP inhibitor section, a cleavable linker, and a chelating agent. It targets specific sites via its disease-targeting part, delivering the PARP inhibitor selectively to tumor cells. Under suitable conditions, the cleavable linker releases the PARP inhibitor to hinder DNA damage repair by inhibiting PARP, while the chelating agent transports a radionuclide for cytotoxic action. This compound is applicable in prostate cancer research.

Cyclic ADP-Ribose (ammonium salt) (cADPR) is an endogenous NAD⁺ metabolite that triggers Ca²⁺ release from ER stores via ryanodine receptors and is synthesized by CD38 and CD157. It may also activate TRPM2 in a temperature-dependent manner. Showing potential in research related in inflammation and immunology.

Cyclic ADP-ribose (cADP-ribose) is a calcium mobilizing nucleotide that is biosynthesized from NAD+ by cADP-ribose synthases, including CD38. cADP-Ribose appears to activate calcium channels in intracellular membranes, which in turn activate ryanodine receptors. 8-bromo-cADP-Ribose is a stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 μM. It is commonly used to investigate intracellular signaling through cADP-ribose in isolated cells and tissues.

ADP-ribose pyrophosphatase is an enzyme that catalyzes the hydrolysis of ADP-ribose into AMP and ribose 5-phosphate.

Endo-1,4-β-xylanase (Xylanase), a glycoside hydrolase enzyme that degrades arabinoxylan (AX), is commonly utilized in biochemical research. It specifically hydrolyzes the β-xylosidic bonds linking two d-xylopyranosyl residues in a β-(1,4) configuration [1].

COH34 analog 1 is a COH34 oxidation analogue that can be used to synthesize active compounds.

PDD00031705 is a benzimidazolone core, cell-inactive Poly (ADP-ribose) glycohydrolase (PARG) inhibitor.

PARG-IN-7 (Example 38) is a Poly ADP-ribose glycohydrolase (PARG) inhibitor with an IC50 of less than 0.1 μM. It reduces the viability of HCC1806-XRCC1 knockdown (KD) cells, exhibiting an IC50 of less than 1 μM. PARG-IN-7 is applicable in cancer research.

MDOLL-0286 is a selective inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), specifically targeting ARH3 with an IC50 value of 2.3 μM. It inhibits the poly(ADP-ribose) hydrolytic activity of ARH3 on cellular substrates and can suppress the DNA damage response. MDOLL-0286 is applicable in cancer research.

PDD00031704 is an inhibitor of poly (ADP-ribose) glycohydrolase (PARG), with an IC50 greater than 60 µM.

Etidaligide sodium is a DNA repair inhibitor designed to prevent the repair of DNA damage in tumor cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase, enzymes that induce the phosphorylation of H2AX and the paralyzation of proteins.

Etidaligide is a DNA repair inhibitor designed to prevent the repair of DNA damage in tumor cells. It also activates DNA-dependent protein kinases (DNA-PK) and poly (ADP-ribose) polymerases, enzymes that promote the phosphorylation of H2AX and the parylation of proteins.

FORX-428 is an oral small-molecule PARG (poly(ADP-ribose) glycohydrolase) inhibitor that interferes with the DNA damage repair process by blocking the degradation of PAR chains, thereby inducing cell death in tumor cells with defects in the DNA damage response (DDR) or under high replicative stress. FORX-428 retains strong antitumor activity in PARP inhibitor-resistant tumor models and is currently in Phase I clinical trials for advanced solid tumors.

PDD00017272 (34f) is a potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG), exhibiting an EC50 value of 4.8 nM in biochemical assays and 9.2 nM in cellular POM.

PDD00017238 demonstrates a robust inhibitory effect on Poly(ADP-ribose) Glycohydrolase (PARG), displaying EC50 values of 40 nM in biochemical assay and 55 nM in cell POM assessment.

pNP-ADPr is a colorimetric substrate used in continuous activity assays for Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3), aiding research on poly(ADP-ribose) polymerase (PARP) enzymes.

JA2131, a small molecular inhibitor targeting Poly(ADP-ribose) Glycohydrolase (PARG), has an IC50 value of 0.4 μM, modulates DNA damage responses, induces replication fork stalling, and leads to cancer cell death.

TFMU-ADPr serves as a versatile substrate for assessing poly(ADP-ribose) glycohydrolase (PARG) activity, enabling direct measurement of total PAR hydrolase activity through the liberation of a fluorophore. Exhibiting exceptional reactivity, generality, stability, and usability, TFMU-ADPr is an effective tool for evaluating small-molecule inhibitors and investigating the regulation of ADP-ribosyl catabolic enzymes in vitro [1].

PARG-IN-4 (compound A) is an orally active and cell-membrane permeable PARG inhibitor (EC50=1.9 nM) that inhibits tumour growth in mice with antitumour activity.

COH34 (1-[(E)-(4-methylphenyl)sulfanyliminomethyl]naphthalen-2-ol) is a selective inhibitor of PARG with an IC50 of 0.37 nM and a Kd of 0.547 μM. COH34 prolongs PARylation at DNA lesions and traps DNA repair factors.

PARG-IN-6 (Compound 2) is an orally bioavailable PARG inhibitor with an IC50 of 0.3 nM. It exhibits significant anticancer activity against cancer cells, with an IC50 of 0.0368 μM for HCC1395 cells. PARG-IN-6 shows potential for research in colon cancer, appendiceal cancer, and pancreatic cancer.