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1418308-27-6

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1418308-27-6 Usage

Description

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.

Pharmacology

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

references

[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.

Check Digit Verification of cas no

The CAS Registry Mumber 1418308-27-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,1,8,3,0 and 8 respectively; the second part has 2 digits, 2 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1418308-27:
(9*1)+(8*4)+(7*1)+(6*8)+(5*3)+(4*0)+(3*8)+(2*2)+(1*7)=146
146 % 10 = 6
So 1418308-27-6 is a valid CAS Registry Number.

1418308-27-6SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 15, 2017

Revision Date: Aug 15, 2017

1.Identification

1.1 GHS Product identifier

Product name 6-Cyano-N-[(4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-1- (3-pentanyl)-1H-indole-4-carboxamide

1.2 Other means of identification

Product number -
Other names -

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1418308-27-6 SDS

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