INCB024360 is a potent and selective inhibitor of IDO1
| Assay . | Enzyme source/cell . | IC50, nM ± SD . |
|---|---|---|
| Enzyme assay | His-tagged human IDO1 | 71.8 ± 17.5 (n = 21) |
| Cell assays | ||
| Tryptophan-to-kynurenine conversion | HeLa | 7.1 ± 0.6 (n = 56) |
| Human DCs | 12.7 ± 1.1 (n = 3) | |
| 293/MSR-human IDO1 | 15.0 ± 3.3 (n = 4) | |
| OCI-M2 human AML cells | 3.4 (n = 2) | |
| THP-1 human AML cells | 22.6 (n = 2) | |
| Primary human AML BMMCs | > 90% at 100nM (n = 2) | |
| 293/MSR-mouse IDO1 | 52.4 ± 15.7 (n = 8) | |
| 293/MSR-mouse IDO2 | > 5000 (n = 8) | |
| 293/MSR-human TDO | > 10 000 (n = 2) | |
| Tryptophan transport | THP-1 | > 30 000 (n = 2) |
| Assay . | Enzyme source/cell . | IC50, nM ± SD . |
|---|---|---|
| Enzyme assay | His-tagged human IDO1 | 71.8 ± 17.5 (n = 21) |
| Cell assays | ||
| Tryptophan-to-kynurenine conversion | HeLa | 7.1 ± 0.6 (n = 56) |
| Human DCs | 12.7 ± 1.1 (n = 3) | |
| 293/MSR-human IDO1 | 15.0 ± 3.3 (n = 4) | |
| OCI-M2 human AML cells | 3.4 (n = 2) | |
| THP-1 human AML cells | 22.6 (n = 2) | |
| Primary human AML BMMCs | > 90% at 100nM (n = 2) | |
| 293/MSR-mouse IDO1 | 52.4 ± 15.7 (n = 8) | |
| 293/MSR-mouse IDO2 | > 5000 (n = 8) | |
| 293/MSR-human TDO | > 10 000 (n = 2) | |
| Tryptophan transport | THP-1 | > 30 000 (n = 2) |
IDO1 indicates Indoleamine 2,3-dioxygenase-1; DC, dendritic cell; AML, acute myeloid leukemia; and BMMC, bone marrow mononuclear cell.