PFI-3

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM*1mL (in DMSO)
ArtNr HY-12409-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
PFI3
Purity
>98%
MW
321373
Formula
C19H19N3O2
Solubility
10 mM in DMSO
Biological Description
PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
IC50 & 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].

Sicherheitsdatenblatt

HY-12409-10mM.pdf

Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 146,43 €
Rabatt: -10,0%
Preis: 131,79 €
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