Table 1 Thermal stabilization of IDH1wt & R132H by substrates, co-factors and compound 1
From: Biostructural, biochemical and biophysical studies of mutant IDH1
IDH1wt + 1 mM indicated substrate | |||||
|---|---|---|---|---|---|
|  | No substrate | Isocitrate | NADP + | NADPH | aKG |
DMSO Only | 52.2 ± 0.1 | 69.3 ± 0.1 | 58.4 ± 0.1 | 65.0 ± 0.1 | 53.7 ± 0.1 |
20 µM compound 1 | 52.5 ± 0.2 | 69.6 ± 0.1 | 58.2 ± 0.2 | 63.7 ± 0.2 | 53.2 ± 0.1 |
ΔTm (°C) | 0.3 | 0.3 | − 0.2 | − 1.3 | − 0.5 |
IDH1R132H + 1 mM indicated substrate | |||||
|  | No substrate | Isocitrate | NADP + | NADPH | aKG |
DMSO Only | 47.9 ± 0.1 | 48.0 ± 0.2 | 51.6 ± 0.1 | 62.1 ± 0.6 | 46.7 ± 0.2 |
20 µM compound 1 | 53.1 ± 0.4 | 52.9 ± 0.4 | 56.0 ± 1.1 | 67.2 ± 0.6 | 52.4 ± 0.1 |
ΔTm (°C) | 5.3 | 4.9 | 4.4 | 5.1 | 5.7 |
