EZH2-IN-1
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1377997-28-8
- 分子式: C27H28ClN5O2
- 分子量:490.00
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
7 μM
Compound: 23
|
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
|
[PMID: 25406853] |
| KARPAS-422 | GI50 |
13.2 μM
Compound: 44
|
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
|
[PMID: 24900844] |
| KARPAS-422 | GI50 |
23 μM
Compound: 44
|
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
|
[PMID: 24900844] |
| KARPAS-422 | GI50 |
24.8 μM
Compound: 44
|
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
|
[PMID: 24900844] |
| KARPAS-422 | GI50 |
70 μM
Compound: 44
|
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
|
[PMID: 24900844] |
| KARPAS-422 | GI50 |
9.1 μM
Compound: 44
|
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
|
[PMID: 24900844] |
化学情報
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CAS 番号 1377997-28-8
-
分子量 490.00
-
分子式 C27H28ClN5O2
-
SMILES
O=C(NC1CC(C)(C)NC(C)(C)C1)C2=CC=C(OC3=CC=CC(C4=CC=NN=C4)=C3C#N)C(Cl)=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)