Potency data for probe TP-040 and control TP-040n
In vitro potency
| Target name | Target information | Species | Assay description | TP-040 | TP-040n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| OGA | Recombinant human protein from transfected Expi293 cells; full-length | Homo sapiens | Enzymatic OGA assay: Production of the fluorescent product was measured every 5 min for 1 h by a SpectraMax Microplate Reader | IC50 = 46 nM | IC50 > 10 µM | PMID: 33404239 |
| HEXB | from placenta (Sigma-Aldrich) | Homo sapiens | Enzymatic HEXB assay: Production of the fluorescent product was measured every 5 min for 1 h by a SpectraMax Microplate Reader | IC50 > 10 µM | PMID: 33404239 |
In cell potency
| Target name | Target information | Species | Assay description | TP-040 | TP-040n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| OGA | human neuroblastoma SH-SY5Y cells; full-length | Homo sapiens | In-cell western assay: Cell-based inhibition of O-GlcNAcase activity: measured increase in the level of O-GlcNAcylated protein in cells. | EC50 = 450 nM | PMID: 33404239 |