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PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM. PFI-3 is a potent, cell-permeable probe capable of displacing ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromatin. Stability measurements confirmed that PFI-3 has a half-life in aqueous solutions exceeding 7 days at 37°C. In long-term experiments, PFI-3 significantly altered gene expression programs that are important for differentiation of stem cells. PFI-3 mimics the effect of Brg1 deletion, resulting in an increase of the repressive H3K27me3 mark at the TSSs and Stat3 binding sites of these genes. PFI-3 has a half-life of >250 h in PBS, pH 7.4, at 20 °C.
Molecular Weight | 321.37 |
Formula | C19H19N3O2 |
CAS Number | 1819363-80-8 |
Solubility (25°C) | DMSO: ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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