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Apoxidole-1

Chemical Structure : Apoxidole-1

CAS No.:

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 reduce cellular kynurenine (Kyn) levels with IC50 of 46.7 in HeLa cells, but does not inhibit IDO1 expression.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Apoxidole-1 is a potent, selective type IV inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), Apoxidole-1 reduce 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.

Physicochemical Properties

M.Wt 596.70
Formula C31H36N2O8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(tert-butyl) 3-ethyl 6-methyl (6R)-6-(1-methyl-1H-indol-2-yl)-1-tosyl-1,2,5,6-tetrahydropyridine-2,3,6-tricarboxylate

References

1. Caitlin Davies, et al. Angew Chem Int Ed Engl. 2022 Oct 4;61(40):e202209374.

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