PFI-3

Research use only, not for human use.

PFI-3 is a potent and cell active BRG/PB1 bromodomains inhibitor with Kd of 54-97 nM.

PFI-3 is a potent and cell active BRG/PB1 bromodomains inhibitor with Kd of 54-97 nM; shows high selectivity over other bromodomains; exposure of embryonic stem cells to PFI-3 led to deprivation of stemness and deregulated lineage specification; markedly enhances the differentiation of trophoblast stem cells; attenuates adipocyte differentiation and dramatically decreases lipid accumulation; a first in class chemical probe for Family VIII bromodomains.

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. 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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PF-6687252 | PF-06687252

Chromatin/Epigenetic

Bromodomain

PB1(5)bromodomains|SMARCA2|SMARCA4

Cancer

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1819363-80-8

321.38

C19H19N3O2

>98% (HPLC)

DMSO: 32.1 mg/mL (100 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

OC1=C(C(/C=C/N2[C@H](C3)CN(C4=NC=CC=C4)[C@H]3C2)=O)C=CC=C1

(E)-1-(2-hydroxyphenyl)-3-((1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)prop-2-en-1-one

(-20℃)

With Ice Pack

≥ 2 years