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EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. EPZ004777 selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes. EPZ004777 suppressed expression of leukemogenic genes such as Hoxa cluster genes and Meis1, and selectively impaired proliferation of MLL-AF10 and CALM-AF10 transformed cells. In vivo administration of EPZ004777 leads to extension of survival in a mouse MLL xenograft model.
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Source | Cell Death Dis (2018). Figure 2. EPZ004777 |
| Method | Bone resorption assay | |
| Cell Lines | RAW264.7 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 60 h | |
| Results | Furthermore, no significant difference was observed between the effects of treatment at 1 and 10 μM of the DOT1L inhibitors. In bone resorption assays, both EPZ5676 and EPZ004777 increased the resorption pit area at 1 and 10 μM concentrations |
| Molecular Weight | 539.67 |
| Formula | C28H41N7O4 |
| CAS Number | 1338466-77-5 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| BIX 01294 Trihydrochloride
BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
| EPZ-5676
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| 3-Deazaneplanocin A
3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM. |
| EPZ004777 hydrochloride
EPZ004777 hydrochloride is the hydrochloride salt of EPZ004777, which is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM. |
| MM-102
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM. |
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