E7449

SKU: orb1302831

Description

E7449 is a potent small molecule inhibitor of PARP1/2 and TNKS1/2, exhibiting low nanomolar IC50 values. It is a valuable research tool for studying DNA damage response and Wnt signaling pathways in both cellular and animal models of oncology and other diseases.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1140964-99-3
• MW: 317.34
• Purity: 97.13%
• Formula: C₁₈H₁₅N₅O
• SMILES: O=c1[nH][nH]c2nc(CN3Cc4ccccc4C3)nc3cccc1c23
• Target: PARP
• Solubility: DMSO:6.4 mg/mL (20.17 mM)

Bioactivity

• Target IC50:
  TNKS2:50 nM (IC50)|PARP1:2 nM (IC50)|PARP2:1 nM (IC50)|TNKS1:50 nM (IC50)
• In Vivo:
  E7449 moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model.
• In Vitro:
  E7449 shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. E7449 traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). E7449 most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). E7449 (10 μM) inhibits Wnt signaling in SW480 cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, PARP2, PARP, PARP1, poly ADP ribose polymerase, inhibit, E 7449, E7449, E-7449, Stenoparib, tankyrase1/2, UNII-9X5A2QIA7C

Compound Identifiers

PubChem CID

135565981