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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- CAS No.: 1377997-28-8
- 화학식: C27H28ClN5O2
- 분자량:490.00
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
제품 설명
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] |
Chemical Information
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CAS No. 1377997-28-8
-
분자량 490.00
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)