ChemicalBook > CAS DataBase List > EI1

EI1

Product Name
EI1
CAS No.
1418308-27-6
Chemical Name
EI1
Synonyms
EI1;CS-2378;EI1;EI 1;KB-145943;EI1 USP/EP/BP;EI1;EI-1;EI 1;EI1 (KB145943;Ezh2 inhibitor;EI1 (Ezh2 inhibitor;Histone Methyltransferase,Inhibitor,inhibit,Apoptosis,EI-1,EI1,KB145943,EI 1,KB 145943
CBNumber
CB52655403
Molecular Formula
C23H26N4O2
Formula Weight
390.48
MOL File
1418308-27-6.mol
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EI1 Property

Boiling point:
675.9±55.0 °C(Predicted)
Density 
1.20±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
insoluble in H2O; insoluble in EtOH; ≥19.5 mg/mL in DMSO
form 
Powder
pka
11.88±0.10(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.00561
Product name
Ezh2 Inhibitor II, EI1 - CAS 1418308-27-6 - Calbiochem
Packaging
10mg
Price
$265
Updated
2024/03/01
Cayman Chemical
Product number
19146
Product name
EI1
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
19146
Product name
EI1
Purity
≥98%
Packaging
5mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
19146
Product name
EI1
Purity
≥98%
Packaging
10mg
Price
$213
Updated
2024/03/01
ChemScene
Product number
CS-1654
Product name
EI1
Purity
99.18%
Packaging
5mg
Price
$95
Updated
2021/12/16
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EI1 Chemical Properties,Usage,Production

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.

EI1 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from EI1 manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
EI1 1418308-27-6
Price
US $0.00-0.00/KG
Min. Order
5mg
Purity
99%HPLC
Supply Ability
2000tons
Release date
2020-01-06

1418308-27-6, EI1Related Search:


  • EI1
  • Ezh2 inhibitor
  • CS-2378
  • EI1 (Ezh2 inhibitor
  • EI1;EI 1
  • 6-Cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide
  • EI1;EI-1;EI 1
  • 6-cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide
  • KB-145943
  • 1H-Indole-4-carboxamide, 6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-
  • EI1 USP/EP/BP
  • EI1 (KB145943
  • Histone Methyltransferase,Inhibitor,inhibit,Apoptosis,EI-1,EI1,KB145943,EI 1,KB 145943
  • 1418308-27-6
  • Inhibitors
  • API