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PFI-3

CAS No. : 1819363-80-8

MCE 站：PFI-3

产品活性：PFI-3是高效，选择性，可渗透细胞的 SMARCA2/4 溴结构域抑制剂，K_d 值为89 nM。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: PFI-3 is a potent, cell-permeable probe capable of displacing ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromatin. PFI-3 binds avidly to both SMARCA2 and SMARCA4 bromodomains (BROMOScan K_d's between 55 and 110 nM) consistent with the binding constant (K_d=89 nM) measured by isothermal titration calorimetry. PFI-3 does not phenocopy the growth inhibitory effects of SMARCA2 knockdown in lung cancer. Exposure of embryonic stem cells to PFI-3 leads to deprivation of stemness and deregulates lineage specification. Furthermore, differentiation of trophoblast stem cells in the presence of PFI-3 is markedly enhanced. PFI-3 binds to certain family VIII bromodomains while displaying significant, broader bromodomain family selectivity. The high specificity of PFI-3 for family VIII is achieved through a novel bromodomain binding mode of a phenolic headgroup that leads to the unusual displacement of water molecules that are generally retained by most other bromodomain inhibitors reported to date.

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