Potency data for probe BTZO-1 and control BTZO-4
In vitro potency
| Target name | Target information | Species | Assay description | BTZO-1 | BTZO-4 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MIF | Recombinant His-tagged (hMIF-His) | Homo sapiens | Scintillation proximity assay (SPA) measurement of selective [3H]-BTZO-1 binding to hMIF-His | Kd = 68.6 nM | ||
| MIF | Rattus sp. | Scintillation proximity assay (SPA) measurement of selective [3H]-BTZO-1 binding to rMIF-His | Kd = 157 nM |
In cell potency
| Target name | Target information | Species | Assay description | BTZO-1 | BTZO-4 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MIF | Homo sapiens | Apoptosis inhibition: MEC1.5: Necessary concentration to give a 50% increase in the viability of rat cardiocytes | MEC1.5 = 16 nM | PMID: 21168764 | ||
| MIF | Homo sapiens | ARE-Luc Reporter Assay (Activation of ARE (antioxidant response element)-mediated cytoprotective gene expression): MEC2.0: Necessary concentration to double luciferase activity in pGL3-ARE-Luc reporter plasmid-transfected H9c2 cells. | MEC2.0 = 820 nM | MEC1.5 > 1 µM | PMID: 21168764 | |
| MIF | Homo sapiens | ARE-Luc Reporter Assay (Activation of ARE (antioxidant response element)-mediated cytoprotective gene expression): MEC2.0: Necessary concentration to double luciferase activity in pGL3-ARE-Luc reporter plasmid-transfected H9c2 cells. | MEC2.0 > 10 µM | PMID: 21168764 |