EPZ-4777
EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research.
For research use only. We do not sell to patients.
- CAS No.: 1381761-52-9
- Formula: C27H40N8O4
- Molecular Weight:540.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
1452 nM
Compound: FED1
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Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis
Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis
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[PMID: 23250418] |
| MOLM-13 | EC50 |
0.004 μM
Compound: 18a, SYC-522
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Antiproliferative activity against human MOLM13 cells containing MLL-AF9
Antiproliferative activity against human MOLM13 cells containing MLL-AF9
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[PMID: 23879463] |
| MV4-11 | EC50 |
0.004 μM
Compound: 18a, SYC-522
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Antiproliferative activity against human MV4-11 cells containing MLL-AF4
Antiproliferative activity against human MV4-11 cells containing MLL-AF4
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[PMID: 23879463] |
| MV4-11 | EC50 |
4.4 μM
Compound: 55
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Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay
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[PMID: 22924785] |
| MV4-11 | IC50 |
0.2 μM
Compound: 4
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Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis
Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis
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[PMID: 23795283] |
| NB-4 | EC50 |
101 μM
Compound: 55
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Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay
Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay
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[PMID: 22924785] |
| THP-1 | EC50 |
0.004 μM
Compound: 18a, SYC-522
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Antiproliferative activity against human THP1 cells containing MLL-AF9
Antiproliferative activity against human THP1 cells containing MLL-AF9
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[PMID: 23879463] |
| THP-1 | EC50 |
8.1 μM
Compound: 55
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Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay
Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay
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[PMID: 22924785] |
EPZ-4777 (1-10000 nM, 24, 72 h) inhibits HOXA9 and LSD1 expression does and time-dependently in MOLM-13 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1381761-52-9
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Molecular Weight 540.66
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Formula C27H40N8O4
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=CN=C3N)O[C@@H]1CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Bon C, et al. Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein. Molecules. 2021 Aug 31;26(17):5300. [Content Brief]
[2]. Lillico R, et al. Selective DOT1L, LSD1, and HDAC Class I Inhibitors Reduce HOXA9 Expression in MLL-AF9 Rearranged Leukemia Cells, But Dysregulate the Expression of Many Histone-Modifying Enzymes. J Proteome Res. 2018 Aug 3;17(8):2657-2667. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EPZ-4777 Related Classifications
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