Potency data for probe TP-060 and control TP-060n
In vitro potency
| Target name | Target information | Species | Assay description | TP-060 | TP-060n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| UGCG | recombinant protein; full length human | Homo sapiens | Human GCS enzymatic assay | IC50 = 31 nM (n=3) | IC50 > 100 µM (n=3) | PMID: 35188773 (T-036) |
| UGCG | recombinant protein; full length mouse | Mus musculus | Mouse GCS enzymatic assay | IC50 = 51 nM (n=3) | IC50 > 100 µM (n=3) | PMID: 35188773 (T-036) |
In cell potency
| Target name | Target information | Species | Assay description | TP-060 | TP-060n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| UGCG | GBA mutant human fibroblasts GM008760 (Coriel Institute); full length human mutated protein | Homo sapiens | Cellular GlcCer reduction: Measured the decrease of GlcCer in fibroblasts obtained from patients with Gaucher’s disease/ molar concentration of glucosylceramide [GlcCer (C16:0)] was quantified using Rapidfire-MS/MS (API-5000, Turbo-ESI, SRM). | EC50 = 7.6 nM (n=3) | EC50 > 10 µM (n=3) | PMID: 35188773 (T-036) |