Sigma-Aldrich Ido Inhibitor - Calbiochem

Assay

≥98% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

DMSO: 50 mg/mL

Storage Temp.

2-8°C

General Description

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).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.

Biochem/Physiol Actions

Cell permeable: noPrimary Target
IDOReversible: yesTarget IC₅₀: 67 nM for hIDO

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Yue, E.W., et al. 2009.J. Med. Chem. 52,7364.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany