PDD00017273

SKU: orb1741484

Description

PDD00017273 is a potent and selective PARG inhibitor that acts as a radiosensitizer. It demonstrates antitumor activity in preclinical models, including in vitro and in vivo studies relevant to epithelial ovarian cancer research.

Research Area

Cell Biology

Key Properties

• CAS Number: 1945950-21-9
• MW: 514.62
• Purity: 99.21% (May vary between batches)
• Formula: C₂₃H₂₆N₆O₄S₂
• SMILES: Cc1cc(Cn2c3ccc(cc3c(=O)n(Cc3cnc(C)s3)c2=O)S(=O)(=O)NC2(C)CC2)n(C)n1
• Target: Poly(ADP-ribose) Glycohydrolase (PARG),Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.89 mM);DMSO:40.83 mg/mL (79.34 mM)

Bioactivity

• Target IC50:
  PARG:1.45 nM (Kd)|PARG:26 nM
• In Vitro:
  PDD 00017273 is an effective inhibitor of PARG with an IC50 of 26 nM and a KD of 1.45 nM. At 10 μM, PDD 00017273 does not inhibit five common cytochrome P450 enzymes. At 30 μM, it moderately increases phosphorylated H2AX (γH2AX) 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.At 0.3 μM, 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PARG, PDD 00017273, PDD00017273, PDD-00017273

Compound Identifiers

PubChem CID

121398766