Chemical Structure : Apoxidole-1
Catalog No.: PC-20021Not For Human Use, Lab Use Only.
Apoxidole-1 is a potent, selective type IV inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), Apoxidole-1 reduces cellular kynurenine (Kyn) levels with IC50 of 46.7 in HeLa cells, but does not inhibit IDO1 expression.
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Apoxidole-1 is a potent, selective type IV inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), Apoxidole-1 reduces cellular kynurenine (Kyn) levels with IC50 of 46.7 in HeLa cells, but does not inhibit IDO1 expression.
Apoxidole-1 targets apo-IDO1 and interferes with heme binding, induces unique amino acid positioning as revealed by crystal structure analysis.
Apoxidole-1 does not inhibit TDO or IDO2.
Apoxidole-1 directly binds to IDO1 with an apparent dissociation constant (KD,app) of 1.1 uM, ITC KD of 20.7 nM.
Apoxidole-1 is inactive in the IDO1 enzymatic assay at 25°C, after preincubation at 37°C Apoxidole-1 dose-dependently decreases IDO1 activity.
M.Wt | 596.70 | |
Formula | C31H36N2O8S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Caitlin Davies, et al. Angew Chem Int Ed Engl. 2022 Oct 4;61(40):e202209374.
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