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PFI-3

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Chemical Structure| 1819363-80-8 同义名 : -
CAS号 : 1819363-80-8
货号 : A455988
分子式 : C19H19N3O2
纯度 : 99%+
分子量 : 321.373
MDL号 : MFCD28100807
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(373.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • bromodomain

    SMARCA2A, Kd:72 nM

    SMARCA4, Kd:55 nM
描述 PFI-3, a potent and cell-permeable probe, effectively displaces ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromatin. It exhibits strong binding to both SMARCA2 and SMARCA4 bromodomains (The KD of the BROMOScan ranges from 55 to 110 nM), consistent with the measured binding constant (KD=89 nM) determined by isothermal titration calorimetry. However, PFI-3 fails to mimic the growth-inhibitory effects observed with SMARCA2 knockdown in lung cancer [1]. Treating embryonic stem cells with PFI-3 results in loss of stemness and disruption of lineage specification. Additionally, PFI-3 significantly boosts the differentiation of trophoblast stem cells [2]. PFI-3 selectively targets specific family VIII bromodomains while maintaining significant overall bromodomain family selectivity. Its unique binding mode, involving a phenolic headgroup, disrupts water molecules typically retained by other bromodomain inhibitors, contributing to its high specificity for family VIII [3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.11mL

0.62mL

0.31mL

15.56mL

3.11mL

1.56mL

31.12mL

6.22mL

3.11mL
参考文献

[1]Vangamudi B, et al. The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies. Cancer Res. 2015 Sep 15;75(18):3865-78.

[2]Fedorov O, et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Sci Adv. 2015 Nov 13;1(10):e1500723.

[3]Gerstenberger BS, et al. Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. J Med Chem. 2016 May 26;59(10):4800-11.