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  • DC Chemicals Limited
  • China
  • Product Name: PFI-3
  • Price: $400.0/100mg $800.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1819363-80-8

1819363-80-8 structure
1819363-80-8 structure
  • Name: PFI-3
  • Chemical Name: PFI-3
  • CAS Number: 1819363-80-8
  • Molecular Formula: C19H19N3O2
  • Molecular Weight: 321.373
  • Catalog: Biochemical Inhibitor Epigenetics Epigenetic Reader Domain Inhibitor
  • Create Date: 2018-02-06 08:30:53
  • Modify Date: 2024-01-08 21:39:34
  • PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.

Name PFI-3
Synonyms 2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)-
(2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-2-propen-1-one
PFI3
Description PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
Related Catalog
Target

Kd: 89 nM (SMARCA2/4)[1]

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 Kd's between 55 and 110 nM) consistent with the binding constant (Kd=89 nM) measured by isothermal titration calorimetry. PFI-3 does not phenocopy the growth inhibitory effects of SMARCA2 knockdown in lung cancer[1]. 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[2]. 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[3].
Kinase Assay To establish whether PFI-3 intercalates DNA, the compound is assessed using a DNA unwinding assay. PFI-3 (1, 5, or 10 μM), cisplatin, or doxorubicin is incubated with supercoiled pBR322, in the presence of wheat germ topoisomerase I, for 30 min at 37°C. DNA incubated with DMSO in the presence or absence of the enzyme is run as control. After extraction by butanol and chloroform/isoamyl alcohol 24:1, the DNA is run in a 1% (w/v) agarose gel with a 1-kb DNA ladder for 4 hours at 80 V. The gel is then stained with SYBR Safe for 30 min before ultraviolet visualization[2].
References

[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.

Density 1.3±0.1 g/cm3
Boiling Point 528.5±50.0 °C at 760 mmHg
Molecular Formula C19H19N3O2
Molecular Weight 321.373
Flash Point 273.4±30.1 °C
Exact Mass 321.147736
LogP 2.19
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.712
Storage condition 2-8°C