A cell-permeable pyrazinopyrimidinecarboxamide that competes against beta-catenin for CBP (CREB-binding protein) binding and selectively prevents CBP- but not p300-, dependent TCF/beta-catenin transcriptional regulations both in cultures in vitro (5 to 25uM) and in mice in vivo (5mg/kg/day via osmotic pump infusion), while not affecting CBP-dependent transcriptional activities mediated by the AP-1 or CRE complex. Shown to reactivate p300//TCF/beta-catenin-mediated neuronal differentiation upon NGF stimulation in PS-1 L286V mutant-expressing PC-12 cultures and be efficacious in alleviating bleomycin- (0,08 units/50 uL/mouse; administered intranasally) induced pulmonary fibrosis in mice.
Molecular Formula:C₃₃H₃₂N₄O₄
Solubility:DMSO
Primary Target:CREB-binding protein
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.