IDO1/TDO-IN-18
IDO1/TDO-IN-18 is a IDO1/TDO inhibitor with an IC50 of 26.54 μM against human IDO1 and an IC50 of 15.63 μM against human TDO. IDO1/TDO-IN-18 targets the apo-forms of IDO1 and TDO to displace the heme cofactor, attenuates the IDO1/SHP-2 interaction, reduces the output of the kynurenine pathway in tumor cells, and inhibits the proliferation and migration of cancer cells. IDO1/TDO-IN-18 can serve as a chemical probe for enzymology and signal transduction-related studies of the IDO1/TDO axis, and can also be used in cancer-related research.
For research use only. We do not sell to patients.
- Formula: C28H27N5O2
- Molecular Weight:465.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hIDO1 26.54 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
1.10 μM
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Inhibition of IFNγ-induced IDO1 activity in human A375 melanoma cells assessed via quantification of kynurenine and tryptophan levels using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio.
Inhibition of IFNγ-induced IDO1 activity in human A375 melanoma cells assessed via quantification of kynurenine and tryptophan levels using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio.
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42483959 |
| HepG2 | IC50 |
1.71 μM
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Inhibition of constitutive TDO activity in human HepG2 hepatocellular carcinoma cells assessed via quantification of kynurenine pathway metabolites using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio under basal (no IFNγ) conditions.
Inhibition of constitutive TDO activity in human HepG2 hepatocellular carcinoma cells assessed via quantification of kynurenine pathway metabolites using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio under basal (no IFNγ) conditions.
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42483959 |
| HepG2 | IC50 |
0.37 μM
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Inhibition of combined constitutive TDO and IFNγ-induced IDO1 activity in human HepG2 hepatocellular carcinoma cells assessed via quantification of kynurenine pathway metabolites using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio.
Inhibition of combined constitutive TDO and IFNγ-induced IDO1 activity in human HepG2 hepatocellular carcinoma cells assessed via quantification of kynurenine pathway metabolites using targeted metabolomics, with inhibition calculated from the Kyn/Trp ratio.
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42483959 |
| A-375 | IC50 |
4.04 μM
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Inhibition of IFNγ-induced IDO1 activity in human A375 melanoma cells under normal conditions assessed via quantification of kynurenine levels using HPLC after 48 h incubation.
Inhibition of IFNγ-induced IDO1 activity in human A375 melanoma cells under normal conditions assessed via quantification of kynurenine levels using HPLC after 48 h incubation.
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42483959 |
| A-375 | IC50 |
1.08 μM
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Inhibition of IFNγ-induced apo-IDO1 activity in human A375 melanoma cells under heme-depleted (succinylacetone treatment) conditions assessed via quantification of kynurenine levels using HPLC after 48 h incubation.
Inhibition of IFNγ-induced apo-IDO1 activity in human A375 melanoma cells under heme-depleted (succinylacetone treatment) conditions assessed via quantification of kynurenine levels using HPLC after 48 h incubation.
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42483959 |
IDO1/TDO-IN-18 binds to apo-IDO1 and displaces the heme cofactor from recombinant human holo-IDO1. It binds to apo-TDO and displaces the heme cofactor from recombinant human holo-TDO, with an apparent IC50 of 15.63 μM[1].
IDO1/TDO-IN-18 does not directly inhibit holo-IDO1; instead, it requires conversion to the apo-form to exert inhibitory activity. As indicated by the observation that inhibitory effects only appear after pre-incubation at 37.5 °C for 120 min, its IC50 under this condition is 26.54 μM. It stabilizes the apo-form of recombinant human IDO1[1].
IDO1/TDO-IN-18 (0.01-30 μM; 48 h) exhibits enhanced inhibitory activity against apo-IDO1 in IFNγ-stimulated A375 cells: its IC50 shifts left to 1.08 μM under heme-depleted conditions compared with 4.04 μM under normal conditions[1].
IDO1/TDO-IN-18 (10 μM; 16 h) inhibits the catalytic activity of IDO1 in SKOV-3 ovarian cancer cells, significantly reducing kynurenine release; it also attenuates the IDO1/SHP-2 signaling axis in SKOV-3 ovarian cancer cells and decreases the interaction between IDO1 and SHP-2[1].
IDO1/TDO-IN-18 (10 μM; 24 h) inhibits migration and wound healing of SKOV-3 ovarian cancer cells[1].
IDO1/TDO-IN-18 is a dual inhibitor of IDO1/TDO. In stably transfected P1.HTR cells, it exhibits an IC50 value of 2.90 μM against human IDO1, 1.47 μM against mouse IDO1, 0.42 μM against human TDO, and 13.11 μM against mouse TDO[1].
IDO1/TDO-IN-18 (compound 66) (incubated for 60 min) shows significantly improved metabolic stability in mouse liver microsomes compared with VS-15 (HY-168092)[1].
IDO1/TDO-IN-18 potently inhibits IFNγ-induced IDO1 activity in A375 melanoma cells (IC50 = 1.10 μM); it suppresses basal TDO activity in HepG2 hepatocellular carcinoma cells and U87 glioblastoma cells with IC50 values of 1.71 μM and 1.02 μM, respectively, and exhibits dual-target inhibition of TDO and IFNγ-induced IDO1 in these two cell lines with IC50 values of 0.37 μM and 1.11 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV-3 ovarian cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly reduced the percentage of migrated cells compared to vehicle-treated and linrodostat-treated controls.
Chemical Information
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Molecular Weight 465.55
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Formula C28H27N5O2
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SMILES
O=C(NCCC1=CNC2=C1C=CC=C2)C3=CC=CC=C3NC(NCCC4=CNC5=C4C=CC=C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IDO1/TDO-IN-18 Related Classifications
HY-187530 Related Classifications
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