PDD 00017273 是一种有效的聚(二磷酸腺苷核糖)水解酶 (PARG) 抑制剂，IC50值为 26 nM，KD值为 1.45 nM。

PDD 00017273 is a potent Poly(ADP-ribose) Glycohydrolase (PARG) inhibitor with an IC 50 of 26 nM and a KD of 1.45 nM [1] [2].

PDD 00017273 is a potent PARG inhibitor, with an IC 50 of 26 nM, and a K D of 1.45 nM. PDD 00017273 (10 μM) does not inhibit five common Cytochrome P450 enzymes. PDD 00017273 (30 μM) modestly increases the intensity of phosphorylated H2AX (γH2AX), PDD 00017273 also decreases in NAD/H through PARG inhibition after DNA damage. PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1 [1]. PDD 00017273 (0.3 μM) inhibits degradation of PAR polymers in MCF7 cells. PDD 00017273 (0.3 μM) also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 stalls replication forks and induces DNA damage that requires homologous recombination (HR) for repair [2].

1945950-21-9

C23H26N6O4S2

514.62

PDD00017273

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years