SMALL MOLECULES
Contributor Information
- Name Allan Jordan ; Kate Smith
- Institute Cancer Research Technology Ltd
Tool Details
- Tool name: PARG inhibitor PDD00031704 Inactive Small Molecule (Tool Compound)
- Alternate names: Poly(ADP-ribose) glycohydrolase
- Molecular formula: C24H28N6O4S2
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: Inhibitor
- Molecular weight of the target: 528.16
- Description: Poly(ADP ribose) glycohydrolase (PARG) has been shown to be a critical component in the repair of single strand DNA breaks. PARG counteracts the function of the ARTD family of poly(ADP ribose) polymerases, commonly known as PARPS, by efficiently catalysing the hydrolysis of O-glycosidic linkages of ADP-ribose polymer, thereby reversing the effects of PARPs. As PARG exists as a single protein, it presents an attractive target for therapeutic intervention in cancer cells with enhanced dependence upon DNA repair. Methylation of the sulphonamide moiety of the PARG Inhibitor PDD00017273 was found to disrupt PARG-binding interactions, rendering the compound inactive and providing useful controls to demonstrate on-target pharmacology of the active compound.
- Research area: Cancer; Fluorescent Cell Imaging
- IC50: >100ÂľM (PARG)
- Additional notes: N-methylated analogs of the PARG tool compounds are inactive.
- For Research Use Only
Target Details
- Target molecular weight: 528.16
- Primary target: Poly(ADP-ribose) glycohydrolase (PARG)
Application Details
Handling
- Purity: 528.16 g/mol
- Storage conditions: Ambient
- Shipping conditions: Dry Ice
Documentation
- Available on request
Related Tools
References
- • 27689388
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