PARG-IN-4

SKU: orb1943219

Description

PARG-IN-4 (Compound A) is a potent, cell-permeable, and orally bioavailable PARG inhibitor with an EC50 of 1.9 nM. This small molecule demonstrates antitumor efficacy in mouse models and is a valuable chemical probe for studying PARP biology, DNA repair mechanisms, and cancer therapeutics in both in vitro and in vivo research.

Research Area

Cell Biology

Key Properties

• CAS Number: 2988890-20-4
• MW: 497.59
• Purity: 98.51% (May vary between batches)
• Formula: C₂₀H₂₅F₂N₇O₂S₂
• SMILES: S(NC1(C)CC1)(=O)(=O)C=2C=C3C(=C(C2)N4C[C@H](C)N[C@@H](C)C4)C=NN3C=5SC(C(F)F)=NN5
• Target: Poly(ADP-ribose) Glycohydrolase (PARG),Apoptosis
• Solubility: DMSO:16 mg/mL (32.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.02 mM)

Bioactivity

• Target IC50:
  HCC1954 cells:0.37 μM|RMUG-S cells:8 nM
• In Vivo:
  In a patient-derived xenograft (PDX) mouse model (HBCx-34), oral administration of PARG-IN-4 (100 mg/kg, once daily for 45 days) led to complete tumor regression, achieving a tumor growth inhibition rate (TGI) of 110%.
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• In Vitro:
  PARG-IN-4 shows strong anti-proliferative effects against ovarian and breast cancer cells. It inhibited cell growth with IC₅₀ values ranging from 8 nM (RMUG-S) to 0.37 μM (HCC1954), depending on the cell line.
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Storage & Handling

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

Compound Identifiers

PubChem CID

169078314