PDD00017273 Inhibitor

99.14%

Powder: -20 degree C for 3 years | In solvent: -80 degree C for 1 year

514.62

C(N1C=2C(C(=O)N(CC3=CN=C(C)S3)C1=O)=CC(S(NC4(C)CC4)(=O)=O)=CC2)C=5N(C)N=C(C)C5

C23H26N6O4S2

DMSO: 20 mg/mL (38.86 mM)
Need ultrasonic
(< 1 mg/ml refers to the product slightly soluble or insoluble)

1945950-21-9

PARG: 1.45 nM (Kd), PARG: 26 nM

PDD 00017273 is an effective Inhibitor of PARG with an IC50 of 26 nM and a KD of 1.45 nM. At 10uM, PDD 00017273 does not inhibit five common cytochrome P450 enzymes. At 30uM, it moderately increases phosphorylated H2AX (gammaH2AX) intensity. Additionally, PDD 00017273 reduces NAD/H through PARG inhibition after DNA damage. The compound inhibits ZR-75-1 cells carrying wild-type BRCA1 and BRCA2 and exhibits weaker activity against MDA-MB-436 cells carrying the 5396 + 1G>A mutation in BRCA1[2].At 0.3uM, PDD 00017273 inhibits the degradation of PAR polymers in MCF7 cells. It also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1-depleted cells. PDD 00017273 halts replication forks and induces DNA damage requiring homologous recombination (HR) for repair[1].