A PARG inhibitor (IC50 = 26 nM in an enzyme assay); maintains persistence of nuclear PAR chains in HeLa cells in the presence of the DNA damaging agent MMS (IC50 = 37 nM); increases nuclear γH2AX intensity in MCF-7 cells in a concentration-dependent manner when used in combination with MMS; reduces clonogenic growth of ZR-75-1 and MDA-MB-436 cells but not HCC1937 cells (IC50s = 0.2

PDD00017273 – 5 mg

Brand:
Cayman
CAS:
1945950-21-9
Storage:
-20
UN-No:
Non-Hazardous - /

PDD00017273 is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor (IC50 = 26 nM in an enzyme assay).{32645} It maintains persistence of nuclear PAR chains in HeLa cells induced by the DNA damaging agent methylmethanesulfonate (MMS; IC50 = 37 nM). PDD00017273, in combination with MMS, increases nuclear phosphorylated H2AX (γH2AX) intensity, a marker of DNA double strand breaks, in MCF-7 cells in a concentration-dependent manner. It reduces clonogenic growth of ZR-75-1 and MDA-MB-436 cells but not HCC1937 cells (IC50s = 0.2, 0.8, and >10 μM, respectively).  

 

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Description

A PARG inhibitor (IC50 = 26 nM in an enzyme assay); maintains persistence of nuclear PAR chains in HeLa cells in the presence of the DNA damaging agent MMS (IC50 = 37 nM); increases nuclear γH2AX intensity in MCF-7 cells in a concentration-dependent manner when used in combination with MMS; reduces clonogenic growth of ZR-75-1 and MDA-MB-436 cells but not HCC1937 cells (IC50s = 0.2, 0.8, and >10 μM, respectively)

Formal name: 1-[(1,3-dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide

Synonyms: 

Molecular weight: 514.6

CAS: 1945950-21-9

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP

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