EPZ-5676
- Pinometostat - EPZ-005676
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C30H42N8O3
- MW: 562.71
Description
EPZ-5676 is a potent, selective and S-adenosyl methionine (SAM) competitive inhibitor of DOT1L methyltransferase (Ki = 80 pM), displaying 37,000-fold selectivity over all other methyltransferases tested. It inhibits H3K79 methylation and MLL-fusion target gene expression, and potently and selectively kills acute leukemia cell lines bearing MLL translocations.
More Information
| Parent CAS No. | 1380288-87-8 |
|---|---|
| Chemical Name | (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-tert-butyl-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | [C@H]1(O)[C@H](N2C=NC3C(N)=NC=NC=32)O[C@H](CN(C(C)C)[C@H]2C[C@@H](CCC3=NC4C=C(C(C)(C)C)C=CC=4N3)C2)[C@H]1O |&1:0,2,14,20,22,39,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17?,19?,22-,25-,26?,29-/m1/s1 |
| InChiKey | LXFOLMYKSYSZQS-IOJWVLQPSA-N |
| CID | 118676762 |
| Short Description | DOT1L histone methyltransferase inhibitor |
References
- SR Daigle et al. Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood. 2013 Aug 8;122(6):1017-25.
- CR Klaus et al. DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56.
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