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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 |
|---|
| (S)-LY-3381916
(S)-LY-3381916 is an active S-isomer of LY-3381916. (S)-LY-3381916 binds to IDOL with an IC50 value less than 1.5 µΜ. LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1. |
| IDO2-IN-1
IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for the research of inflammatory autoimmunity. |
| IDO1/2-IN-1
IDO1/2-IN-1 is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. |
| IDO1/2-IN-1 hydrochloride
IDO1/2-IN-1 hydrochloride is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. |
| IDO-IN-18
IDO-IN-18 is an IDO inhibitor. |
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