PFI 3
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Description: Potent and selective SMARCA2/4 and polybromo 1 inhibitor
Chemical Name: (2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
Purity: ≥98%
Biological Activity
Potent and selective polybromo 1 and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively). Also inhibits SMARCA2. Displays 30-fold selectivity over other sub-family branches. Accelerates FRAP recovery in cells at a concentration of 1 μM.Technical Data
M.Wt:
321.37
Formula:
C19H19N3O2
Solubility:
Soluble to 100 mM in DMSO and to 5 mM in ethanol with gentle warming
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1819363-80-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 3 probe summary on the SGC website.
Background References
-
Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit.
Gerstenberger et al.
J.Med.Chem., 2016;59:4800 -
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
Vangamudi et al.
Cancer Res., 2015;75:3865
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