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
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
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..…
N-Bromosuccinimide Price
- Product number
- 5.00561
- Product name
- Ezh2 Inhibitor II, EI1 - CAS 1418308-27-6 - Calbiochem
- Packaging
- 10mg
- Price
- $265
- Updated
- 2024/03/01
- Product number
- 19146
- Product name
- EI1
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 19146
- Product name
- EI1
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 19146
- Product name
- EI1
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $213
- Updated
- 2024/03/01
- Product number
- CS-1654
- Product name
- EI1
- Purity
- 99.18%
- Packaging
- 5mg
- Price
- $95
- Updated
- 2021/12/16
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
EI1 Suppliers
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- Fax
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- Country
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View Lastest Price from EI1 manufacturers
- 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