ZY-MY-111
Based on 1 Customer Validation
ZY-MY-111 is a selective interleukin-4-induced-1 (IL4I1) inhibitor (IC50 = 1.86 μM). ZY-MY-111 competitively occupies the catalytic pocket of IL4I1 and disrupts Trp-AHR signaling in cells. ZY-MY-111 promotes T cell proliferation, enhancing immune responses against the tumor cells. ZY-MY-111 can be used to study colon carcinoma and lymphoma.
For research use only. We do not sell to patients.
- Formula: C16H14ClFN2S
- Molecular Weight:320.81
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
IL4I1 1.86 μM (IC50) |
In Vitro
ZY-MY-111 (30 min) exhibits potent and selective inhibition against IL4I1 with an IC50 of 1.86 μM, while showing no inhibition of IDO1-mediated tryptophan metabolism even at 10 μM[1].
ZY-MY-111 (100 μM) shows stable binding to IL4I1, as demonstrated by a significant thermal shift (ΔTm = 4.5 °C) at 100 μM in thermal shift assay[1].
ZY-MY-111 (5.6 μM; 30 min) reversibly binds to IL4I1, as evidenced by time-dependent attenuation of its inhibitory activity in dialysis assays[1].
ZY-MY-111 (1.25-20 μM; 30 min) exhibits concentration-dependent effects on IL4I1-mediated oxidative deamination kinetics in substrate titration experiments[1].
ZY-MY-111 (1.25-20 μM; 30 min) shows mixed-type inhibition of IL4I1, with increasing Km and decreasing Vmax at higher concentrations, indicating dual binding to the catalytic site and an allosteric pocket[1].
ZY-MY-111 (24 h) dose-dependently suppresses basal AHR activation with an IC50 of 2.14 μM and compromises tryptophan-induced AHR signaling at 148 μM L-tryptophan co-treatment in HEK293T-XRE reporter cells[1].
ZY-MY-111 (1.25-10 μM; 36 h) suppresses CYP1A1 expression and this effect is attenuated in IL4I1-knockdown cells, confirming that its inhibition of AHR signaling is dependent on IL4I1 in HEK293T-XRE reporter cells[1].
ZY-MY-111 (1.25-5 μM; 36 h) suppresses key AHR pathway genes, and this effect is diminished when IL4I1 levels are reduced in HEK293T-XRE reporter cells[1].
ZY-MY-111 (10 μM; 24 h) significantly suppresses L-tryptophan (HY-N0623) (500 μM)-induced AHR nuclear accumulation and rescues the up-regulation of CYP1A1 expression in HT-29 cells[1].
ZY-MY-111 (2.5-20 μM; 72 h) dose-dependently restores CD8⁺ T cell proliferation in anti-CD3/CD28-activated hPBMCs at 1-20 μM, and this effect is completely abrogated by I3P and reversed by IL4I1-conditioned media blockade at 10 μM[1].
ZY-MY-111 (0.8-2.5 μM; 144 h) dose-dependently enhances the anti-tumor function of cytotoxic T cells, as revealed by quantification of tumor cell viability in GFP-expressing HT-29 cancer cells and anti-CD3/CD28-activated hPBMCs[1].
ZY-MY-111 (3 days) shows no significant direct inhibitory effect on the growth or viability of A20 or CT26 tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ZY-MY-111 (25 mg/kg; i.p.; twice a day) significantly suppresses CT26 tumor growth and remodels the immunosuppressive tumor microenvironment by blocking the IL4I1 signaling pathway, as evidenced by increased CD8⁺/CD4⁺ T cell ratio and effector memory T cell infiltration, along with reduced MDSCs and Treg frequencies in CT26 colon carcinoma-bearing mice[1].
ZY-MY-111 (50 mg/kg; i.p.; twice a day) shows no significant antitumor efficacy in immunodeficient NU/NU nude mice bearing CT26 tumors, suggesting that its tumor growth inhibition depends on T cell-mediated immune responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (6–8 weeks old) were subcutaneously injected with 1 × 106 A20 B lymphoma cells in a 1:1 mixture of PBS and Matrigel in the right flank[1].
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Dosage:50 mg/kg
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Administration:i.p.; twice a day
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Result:Significantly suppressed tumor growth.
Increased the CD8⁺/CD4⁺ T cell ratio in tumor-infiltrating lymphocytes.
Induced a CD8⁺ T cell-mediated antitumor effect.
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Animal Model:Female BALB/c mice (6–8 weeks old) were subcutaneously injected with 1 × Female BALB/c mice (6–8 weeks old) were subcutaneously injected with 5 × 10⁵ CT26 colon carcinoma cells in the right flank[1].
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Dosage:25 mg/kg
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Administration:i.p.; twice a day
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Result:Significantly suppressed CT26 tumor growth.
Remodeled the immunosuppressive tumor microenvironment by blocking the IL4I1 signaling pathway.
Increased the CD8⁺/CD4⁺ T cell ratio in tumor-infiltrating lymphocytes.
Enhanced effector memory T cell infiltration.
Reduced MDSCs and Treg frequencies.
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Animal Model:Female NU/NU nude mice (6–8 weeks old) were subcutaneously injected with 5 × 10⁵ CT26 colon carcinoma cells in the right flank[1].
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Dosage:50 mg/kg
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Administration:i.p.; twice a day
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Result:Did not significantly inhibit tumor growth.
Showed no significant antitumor efficacy.
Failed to suppress tumor growth in the absence of T cells, suggesting that its antitumor effect depends on T cell-mediated immune responses.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Research Protocol for Cancer Immunology
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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Appearance Solid
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Molecular Weight 320.81
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Formula C16H14ClFN2S
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Color White to off-white
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SMILES
FC1=CC=C2NC(N(CC2=C1)CCC3=CC(Cl)=CC=C3)=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (311.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (15.59 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1171 mL | 15.5855 mL | 31.1711 mL | 77.9277 mL |
| 5 mM | 0.6234 mL | 3.1171 mL | 6.2342 mL | 15.5855 mL | |
| 10 mM | 0.3117 mL | 1.5586 mL | 3.1171 mL | 7.7928 mL | |
| 15 mM | 0.2078 mL | 1.0390 mL | 2.0781 mL | 5.1952 mL | |
| 20 mM | 0.1559 mL | 0.7793 mL | 1.5586 mL | 3.8964 mL | |
| 25 mM | 0.1247 mL | 0.6234 mL | 1.2468 mL | 3.1171 mL | |
| 30 mM | 0.1039 mL | 0.5195 mL | 1.0390 mL | 2.5976 mL | |
| 40 mM | 0.0779 mL | 0.3896 mL | 0.7793 mL | 1.9482 mL | |
| 50 mM | 0.0623 mL | 0.3117 mL | 0.6234 mL | 1.5586 mL | |
| 60 mM | 0.0520 mL | 0.2598 mL | 0.5195 mL | 1.2988 mL | |
| 80 mM | 0.0390 mL | 0.1948 mL | 0.3896 mL | 0.9741 mL | |
| 100 mM | 0.0312 mL | 0.1559 mL | 0.3117 mL | 0.7793 mL |
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