EI1 |
| رقم الكتالوجGC14756 |
EI1 (KB-145943) هو مثبط EZH2 فعال وانتقائي مع IC50 من 15 نانومتر و 13 نانومتر لـ EZH2 (WT) و EZH2 (Y641F) ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1418308-27-6
Sample solution is provided at 25 µL, 10mM.
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IC50: 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
EI1 performs as a highly potent inhibitor of Ezh2 which is named enhancer of zeste homolog 2. Mutation and over-expression of Ezh2 has been linked to the development of cancer. Since Ezh2 is upregulated in multiple cancers, it seems to play a crucial role in the regulation of tumor angiogenesis and has been considered as a potential target in anticancer therapy. Ezh2 stimulates cancer development by inhibiting tumor-suppressing genes. Suppressing Ezh2 activity may therefore inhibit tumor growth. [1]
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]
In vivo: So far, no in vivo study has been conducted.
Clinical trial: So far, no clinical trial has been conducted.
Reference:
[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.
| Cell experiment [1]: | |
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Cell lines |
Ezh2 mutant diffused large B-cell lymphoma (DLBCL) cells, Ezh2 wild-type DLBCL cells and mouse embryonic fibroblasts (MEFs) |
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Preparation method |
The solubility of this compound in DMSO is > 19.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10 μM; 11 ~ 15 days |
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Applications |
In DLBCL cells, EI1 inhibited the methylation of cellular lysine 27 of histone H3 (H3K27), and up-regulated the expression of Ezh2 target gene p16. In MEFs, EI1 inhibited H3K27me3 and cell proliferation. In DLBCL cells carrying Ezh2 mutation, EI1 selectively inhibited cell growth, as well as induced cell cycle arrest and apoptosis. |
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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. |
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| Cas No. | 1418308-27-6 | SDF | |
| Chemical Name | 6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide | ||
| Canonical SMILES | CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C | ||
| Formula | C23H26N4O2 | M.Wt | 390.48 |
| الذوبان | ≥ 19.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.561 mL | 12.8048 mL | 25.6095 mL |
| 5 mM | 0.5122 mL | 2.561 mL | 5.1219 mL |
| 10 mM | 0.2561 mL | 1.2805 mL | 2.561 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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