EI1

Bezeichnung:EI1

CAS-Nr1418308-27-6

Englisch Name:EI1

CBNumberCB52655403

SummenformelC23H26N4O2

Molgewicht390.48

MOL-Datei1418308-27-6.mol

EI1 physikalisch-chemischer Eigenschaften

Siedepunkt	675.9±55.0 °C(Predicted)
Dichte	1.20±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	insoluble in H2O; insoluble in EtOH; ≥19.5 mg/mL in DMSO
Aggregatzustand	Powder
pka	11.88±0.10(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

EI1 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
EZH2 is a histone methyltransferase and its activation leads to alteration in cell cycle regulation, proliferation, and cancer progression [65]. High expression and mutation of EZH2 are in a variety of malignancies and usually portend for a poor prognosis.
Pharmakologie
EZH2 has been shown to repress the cell cycle inhibitor p21 and other proapoptotic factors, thereby promoting cell cycling in SCLC cells. In various SCLC cell lines, suppression of EZH2 leads to reduction of cells in S, G2/M phase with increased p21 expression. EZH2 was also shown to prevent apoptosis by inhibition of TGF-β via histone methyltransferase methylation of lysine 27?in histone H3 (H3K27me3). In addition, it has been shown that in platinum-resistant cancer cells, protein and mRNA expression EZH2 is upregulated and by silencing EZH2 overcomes drug resistance, making EZH2 a target of interest in SCLC.
in vitro
based on studies from dlbcl cells, it was shown that ei1 suppressed cellular h3k27 methylation and activated expression of ezh2 target gene - p16. ei1 also blocked h3k27 methylation and cell proliferation in mouse embryonic fibroblasts. in addition, ei1 potently and selectively inhibited the growth of dlbcl cells carrying ezh2 mutation, and therefore resulted in cell cycle arrest and apoptosis. [1]
IC 50
a potent and selective suppressor of ezh2 with ic50 values of 15 nm and 13 nm for wild type ezh2 and ezh2 y641f mutant, respectively
Einzelnachweise
[1]qia w, chan hm, teng l, li l, chuai s, zhang rp, zeng j, li m, fan h, lin y, gu j, ardayfiob o, zhang jh, yan x, fang j, mi y, zhang m, zhou t, feng g, chen zj, li g, yang t, zhao k, liu x, yu z, lu cx, atadja p and li e. selective inhibition of ezh2 by a small molecule inhibitor blocks tumor cells proliferation. proc natl acad sci. 2012 dec; 109(52): 213605.

EI1 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1418308-27-6, EI1 Verwandte Suche:

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