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SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.
| Molecular Weight | 618.57 |
| Formula | C28H40BrN7O4 |
| CAS Number | 1561178-17-3 |
| Solubility (25°C) | 33 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| VTP50469
VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL Interaction with a Ki value of 104 pM. VTP50469 has anti-leukemia activity. |
| BIX 01294 Trihydrochloride
BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
| EBI-2511
EBI-2511 is an orally active, potent inhibitor of EZH2 in Pfeffiera cells IC50 The value is 6 nM. |
| EPZ-5676
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| EPZ004777
EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. |
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