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Product Information:

PDD00017272

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[1][2].

Cat. No.: EX-A14640    Purity: >98%
Chemical
Chemical structure of PDD00017272


For research only, Do not use for Human!

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CAS No.1945950-20-8
Purity>98%
FormulaC23H25N5O4S3
Mol Weight531.671
 
 
Reference:  

[1]. Nie L, et al. DePARylation is critical for S phase progression and cell survival. Elife. 2024 Apr 5;12:RP89303.

[2]. Bohdan Waszkowycz, et al. Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides. J Med Chem. 2018 Dec 13;61(23):10767-10792.

CoACoA of PDD00017272
Smiles:CC1=C(SC(=N1)C)CN2C3=C(C=C(C=C3)S(=O)(=O)NC4(CC4)C)C(=O)N(C2=O)CC5=CN=C(S5)C

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