EI1
Based on 2 publication(s) in Google Scholar
EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
For research use only. We do not sell to patients.
- Purity : 98.84%
- CAS No.: 1418308-27-6
- Formula: C23H26N4O2
- Molecular Weight:390.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) EI1
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
EZH2 Y641F mutant type 13 nM (IC50) |
EZH2 WT 15 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
13 nM
Compound: 20, EI1
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Inhibition of N-terminal FLAG tagged human EZH2 Y641F mutant expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by mass spectrophotometric analysis
Inhibition of N-terminal FLAG tagged human EZH2 Y641F mutant expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by mass spectrophotometric analysis
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[PMID: 25406853] |
| Sf9 | IC50 |
15 nM
Compound: 20, EI1
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Inhibition of N-terminal FLAG tagged full-length human EZH2 expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by mass spectrophotometric analysis
Inhibition of N-terminal FLAG tagged full-length human EZH2 expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by mass spectrophotometric analysis
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[PMID: 25406853] |
In Vitro
In DLBCL cells, EI1 (KB-145943) inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression. In mouse embryonic fibroblasts, EI1 (KB-145943) also inhibit H3K27me3 and cell proliferation. In addition, EI1 (KB-145943) selectively inhibits the growth of DLBCL cells carrying Ezh2 mutation, and causes cell cycle arrest and apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1418308-27-6
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Appearance Solid
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Molecular Weight 390.48
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Formula C23H26N4O2
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Color White to off-white
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SMILES
CCC(CC)N(C=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C#N)=C2
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Synonyms
KB-145943
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Eur J Med Res
NF-κB-mediated enhancement of H3K27me3 through EZH2: a mechanism to suppress pyocyanin-induced autophagy in macrophages. [Abstract]2025 Apr 29;30(1):346. PMID: 40301947
Solvent & Solubility
In Vitro:
DMSO : 7.69 mg/mL (19.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5610 mL | 12.8048 mL | 25.6095 mL | 64.0238 mL |
| 5 mM | 0.5122 mL | 2.5610 mL | 5.1219 mL | 12.8048 mL | |
| 10 mM | 0.2561 mL | 1.2805 mL | 2.5610 mL | 6.4024 mL | |
| 15 mM | 0.1707 mL | 0.8537 mL | 1.7073 mL | 4.2683 mL |
EI1 Related Classifications
HY-15573 Related Classifications
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