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PFI-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PFI-3图片
CAS NO:1819363-80-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)321.37
FormulaC19H19N3O2
CAS No.1819363-80-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 64 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES OC1=C(C(/C=C/N2[C@H](C3)CN(C4=NC=CC=C4)[C@H]3C2)=O)C=CC=C1
Synonyms PFI 3; PFI3; PFI-3
实验参考方法
In Vitro

In vitro activity: PFI-3 shows a significant selectivity for PB1(5) and SMARCA2/4 over 36 other tested kinases.


Kinase Assay: Using recombinant purified bromodomains, we discovered that PFI-3 binds with similar avidity to both the short and long isoform of SMARCA2 revealing that the alternatively-spliced 18 amino acid insert does not impair PFI-3 binding. Moreover, profiling against 32 bromodomains at DiscoveRx confirmed exquisite selectivity vs. other subfamilies expanding the PFI-3 selectivity information obtained using differential scanning fluorimetry (DSF). In summary, we find there is a good concordance between the ligand competition (BROMOScan) and the direct biophysical binding (DSF) assays and note that in addition to targeting SMARCA2/4, PFI-3 also has activity (~70% inhibition at 2 uM) against the structurally related fifth bromodomain from PBRM1, another SWI/SNF subunit.


Cell Assay: In cell-based chromatin binding assays, using in situ cell extraction techniques to remove non-chromatin bound proteins, we observed dose-dependent displacement of GFP-tagged SMARCA2 bromodomain (i.e. 132 amino acid residues) by PFI-3. Notably, the inhibitor showed prolonged cell-target engagement with similar potency (IC50 = 5.78 uM) following 2 and 24 hours treatment. As a negative control, JQ1 did not inhibit the binding of ectopically expressed SMARCA2 bromodomain, but selectively displaced GFP-tagged BRD4 (data not shown). Taken together, our cell-biochemical data cooperate the accelerated fluorescence recovery after photobleaching (FRAP) reported for PFI-3 and we conclude that PFI-3 is a selective, cell-permeable probe suitable to study the inhibition of SMARCA2/4 bromodomains in cells.

In Vivo
Animal model
Formulation & Dosage
References

Cancer Res. 2015 Sep 15; 75(18): 3865–3878.