Molecular Formula | C21H33F3N8O7 |
Molar Mass | 566.54 |
Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
In vitro study | 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 (K i =14±6 nM and 345±36 nM, respectively). |
biological activity | GSK2807 Trifluoroacetate is SMYD3 effective and selective, SAM competitive inhibitor with Ki value of 14 nM and IC50 of 130 nM. |
target | SMYD3 14 nM (Ki) SMYD3 130 nM (IC 50 ) |
in vitro study | 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 (K I = 14±6 nM and 345±36 nM, respectively). |