IDO Inhibitor

Cell permeable: no

Primary Target
IDO

Reversible: yes

Target IC₅₀: 67 nM for hIDO

Toxicity: Standard Handling (A)

A cell-permeable, bioactive, non-toxic oxadiazolohydroxyamidine based compound that acts as a potent, selective and competitive inhibitor of indoleamine 2,3-dioxygenase (IDO; IC₅₀ = 67 nM for hIDO). Reversibly binds to the catalytically active heme iron (Fe²⁺) and is inactive towards closely related tryptophan 2,3-dioxygenase (TDO; IC₅₀ >10 µM). Shown to dose-dependently decrease kynurenine levels (IC₅₀ = 19 & 46 nM in HeLa treated with IFN-γ & B16-GM-CSF melanoma cells, respectively) and suppress B16-GM-CSF xenograft tumor growth in C57BL/6 mice (75 mg/kg, s.c., b.i.d.). Though orally bioavailable, but undergoes a rapid clearance (t_1/2<0.5 h).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Yue, E.W., et al. 2009. J. Med. Chem.52, 7364.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany