BTZO-1
| Target | MIF |
| Targeted domain | Tautomerase domain |
| Mode of action | ARE Activator |
| Control | BTZO-4 |
| Recommended cellular usage concentration | 0.8 - 1 µM |
| In vivo use | No |
| Synonyms | TP-010 |
| Donated by | Takeda |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: [3H]-BTZO-1 binds to hMIF and rMIF in SPA binding assay with Kd = 68.6 nM and Kd = 157 nM, respectively |
| Selectivity within target family: > 30-fold | Surpasses criterion: Selectivity against recently discovered D-Dopachrome Tautomerase (DDT) is unknown. |
| Selectivity outside target family | Surpasses criterion: No relevant activity in panel of 280 kinases at 1 µM; KINOMEScan with 468 targets at 1 µM: Closest off-targets of primary data (% Ctrl) are CDK8 (36) and EIF2AK4 (47).Clean PDSP scan with one hit on GABAA/BZP (Ki = 934 nM) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: ARE-Luc Reporter Assay (Activation of ARE (antioxidant response element)-mediated cytoprotective gene expression): MEC2.0 = 820 nM (MEC2.0: Necessary concentration to double luciferase activity in pGL3-ARE-Luc reporter plasmid-transfected H9c2 cells.); Apoptosis inhibition: MEC1.5 = 16 nM (MEC1.5: Necessary concentration to give a 50% increase in the viability of rat cardiocytes) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: ARE-Luc Reporter Assay (Activation of ARE (antioxidant response element)-mediated cytoprotective gene expression): MEC2.0 > 10 µM; Apoptosis inhibition: MEC1.5 > 1 µM; Clean PDSP scanKINOMEScan with 468 targets at 1 µM: Closest off-targets of primary data (% Ctrl) is EIF2AK4 (42). |