AG-14361

• Background:

  A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells.

• Description:

  AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.

• Purity:

  ≥ 98% by HPLC

• Solubility:

  Soluble in DMSO. Solubility in water or ethanol is <1 mg/mL

• Molecular Formula:

  C19H20N4O

• Shipping Conditions:

  Room Temperature (continental US) or Gel Packs

• Storage Conditions:

  Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

• Calculated Molecular Weight:

  320.4 Da

• CAS Number:

  328543-09-5