Table 1. Inhibition data of GlcNAcstatins A–E and PUGNAc against lysosomal HexA/HexB, hOGA and the compounds selectivity for hOGA.
Compound | Hex A/B, Ki (nM)* | hOGA, Ki (nM) | Selectivity (GH20/hOGA) |
---|---|---|---|
GlcNAcstatin A | 0.55±0.05 | 4.3±0.2 | n.s. |
GlcNAcstatin B | 0.17±0.05 | 0.42±0.06 | n.s. |
GlcNAcstatin C | 550±10 | 4.4±0.1 | 164 |
GlcNAcstatin D | 2.7±0.4 | 0.74±0.09 | 4 |
GlcNAcstatin E | 1100±100 | 8500±300 | n.s. |
PUGNAc | 25±2.5 | 35±6* | n.s. |
*The Cheng–Prusoff equation {Ki=IC50/1+([S]/Km)} was used to convert the IC50 values into an absolute inhibition constant (Ki).