GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.
 |
Source | PLoS Pathog (2018). Figure 4. GSK343 |
| Method | ChIP-Seq | |
| Cell Lines | Mice | |
| Concentrations | 10 μM | |
| Incubation Time | - | |
| Results | Additionally, for GSK343, there was a dose-dependent decrease in transformation efficiency, as there was a significant difference (p<0.005) in transformation efficiencies between the 0.4 μM (21% fully transformed) and 2 μM (17% fully transformed) cultures |
| Molecular Weight | 541.69 |
| Formula | C31H39N7O2 |
| CAS Number | 1346704-33-3 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Dongyou Yue, et al. EZH2 inhibitor GSK343 inhibits sepsis-induced intestinal disorders
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