Table 2. Covalent MIF inhibitors and MIF inhibitors with other structures.
Class | Compound | Structure | Activity, μM Reference(s) |
---|---|---|---|
phenyl-pyrimidine | 4-IPP | IC50 = 0.2-0.5 [51] (TA) | |
isothiocyanate | BITC | IC50 = 0.79 [53] (TA) | |
benzoxazinone | NVS-2 | IC50 = 0.020 [55] (TA); Ki = 0.027 [50] (TA); Kd = 0.055 [50] (BA) | |
benzoxazol-2-one | MIF098 (Alissa-5) | IC50 = 0.01 [56] (TA) | |
pyrimidazole | K664-1 | IC50 = 0.11 [59] (TA); Ki = 45 [40] (TA), Ki = 0.16 [58] (TA) | |
chromene | T-614 | IC50 = 6.81 [58] (TA) | |
Kok-10 | IC50 = 18 [60] (TA) | ||
Kok-17 | IC50 = 6.2 [60] (TA) | ||
isoxazoline | CPSI-2705 | 2-10-fold more potent than ISO-1 [35] (TA) | |
CPSI-1306 | 100-fold more potent than ISO-1 [35] (TA) | ||
isocoumarin | SCD-19 | 100% inhibition at concentration of 100 μM [37] (TA) |
TA, tautomerase assay; BA, binding assay MIF-CD74k