Dot1L-IN-1
Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively.
For research use only. We do not sell to patients.
- CAS No.: 2088518-50-5
- Formula: C32H36ClN9O2S
- Molecular Weight:646.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
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DOT1L |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
3 nM
Compound: 7
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Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
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[PMID: 28337327] |
| MV4-11 | IC50 |
5 nM
Compound: 7
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
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[PMID: 28337327] |
Dot1L-IN-1 (analogue 7) effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50=5 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2088518-50-5
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Molecular Weight 646.21
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Formula C32H36ClN9O2S
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SMILES
CC1=NC=CC=C1C2=C(Cl)SC3=CC=C(NC(NCC(NCCCN(C)[C@@H]4CCCN(C5=C(C=CN6)C6=NC=N5)C4)=O)=O)C=C32
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)