1418308-27-6 Usage
Description
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide is a complex organic compound with a molecular structure that features a cyano group, a pyridine ring, and an indole ring. It is characterized by its potential biological activities and applications in various fields.
Uses
Used in Pharmaceutical Industry:
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide is used as a potential therapeutic agent for targeting EZH2, a histone methyltransferase involved in cell cycle regulation, proliferation, and cancer progression. Its application is based on its ability to inhibit EZH2 activity, which is often overexpressed and mutated in various malignancies, leading to a poor prognosis.
Used in Drug Development:
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide is used as a lead compound in the development of novel drugs aimed at treating cancers with high EZH2 expression and mutation levels. Its application is due to its potential to modulate the activity of EZH2, thereby disrupting cancer cell growth and progression.
Used in Chemical Research:
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide is used as a research tool in the study of the structure-activity relationship of EZH2 inhibitors. Its application is based on its unique molecular structure, which can provide insights into the design and optimization of more potent and selective inhibitors targeting EZH2.
Used in Drug Delivery Systems:
6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide can be used as an active pharmaceutical ingredient in the development of drug delivery systems, such as nanoparticles or liposomes, to improve its bioavailability, delivery, and therapeutic outcomes in cancer treatment.
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.
