| Bioactivity | GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM[1][2]. |
| Invitro | A high-resolution crystal structure reveals that GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 is 24-fold selective for SMYD3 in comparison with the closely related enzyme SMYD2 (Ki=14±6 nM and 345±36 nM, respectively)[1]. |
| Name | GSK2807 Trifluoroacetate |
| CAS | 2245255-66-5 |
| Formula | C21H33F3N8O7 |
| Molar Mass | 566.53 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Van Aller GS, et al. Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets. Structure. 2016 May 3;24(5):774-781. [2]. Kaniskan HÜ, et al. Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev. 2018 Feb 14;118(3):989-1068. |
GSK2807 Trifluoroacetate
CAS: 2245255-66-5 F: C21H33F3N8O7 W: 566.53
GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 o
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.