For research use only. Not for therapeutic Use.
DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, where it catalyzes mono-, di-, and trimethylation. Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation. EPZ004777 is a potent inhibitor of DOT1L (IC<sub>50</sub> = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells <em>in vitro</em> and prolongs survival in an MLL xenograft mouse model. It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases. DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.
| Catalog Number | R065218 |
| Synonyms | 7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, monoformic acid salt |
| Molecular Formula | C28H41N7O4 • CH2O2 |
| Purity | ≥95% |
| Storage | -20°C |
| InChI | InChI=1S/C28H41N7O4.CH2O2/c1-17(2)34(13-6-12-30-27(38)33-19-9-7-18(8-10-19)28(3,4)5)15-21-22(36)23(37)26(39-21)35-14-11-20-24(29)31-16-32-25(20)35;2-1-3/h7-11,14,16-17,21-23,26,36-37H,6,12-13,15H2,1-5H3,(H2,29,31,32)(H2,30,33,38);1H,(H,2,3)/t21-,22-, |
| InChIKey | CTNCHYJQYACUDR-XRJUUMFPSA-N |
| SMILES | CC(C)(C)C1=CC=C(NC(NCCCN(C(C)C)C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C=CC4=C3N=CN=C4N)O2)=O)C=C1.[H]C(O)=O |
| Reference | 1.Bernt, K.M., and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias. Epigenomics 3(6), 667-670 (2011). |
