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The IDO inhibitor 1-methyl-tryptophan exists in two stereoisomers with potentially different biological properties. The L isomer is the more potent inhibitor of IDO activity using the purified enzyme and in HeLa cell–based assays. However, the D isomer is significantly more effective in reversing the suppression of T cells created by IDO-expressing dendritic cells. Indoximod (D-1MT, NLG8189) inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Oral administration of dl-1-methyl-tryptophan in combination with paclitaxel can elicit regression of autochthonous breast tumors.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | B16F10 and 4T1 tumor models mice |
| Formulation | - |
| Dosages | 400 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 218.25 |
| Formula | C12H14N2O2 |
| CAS Number | 110117-83-4 |
| Solubility (25°C) | Water 3 mg/mL (ultrasonic and adjust pH to 2 with HCl) DMSO 1 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IDO Products |
|---|
| IDO-IN-2 (NLG-919 Analogue)
NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM. |
| IDO5L
IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM. |
| Coptisine
Coptisine, an alkaloid isolated from Coptis, is an effective non-competitive IDO inhibitor with Ki value of 5.8 μM and IC50 value of 6.3 μM. |
| Coptisine chloride
Coptisine chloride is an effective and non-competitive IDO inhibitor with Ki value of 5.8 μM and IC50 value of 6.3 μM. Coptisine chloride is an effective H1N1 neuraminidase (NA-1) inhibitor with IC50 of 104.6 μg/mL, which can be used for influenza A virus (H1N1) infection. |
| Coptisine-Sulfate
Coptisine Sulfate is an alkaloid isolated from coptis coptidis. It is an effective non-competitive IDO inhibitor with Ki value of 5.8 μM and IC50 value of 6.3 μM. |
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