SHMT2-IN-1
Based on 1 publication(s) in Google Scholar
SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 (SHMT2) inhibitor with an IC50 of 1.21 μM and a KD of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC50 of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer.
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- Pureté : 99.84%
- Formule: C26H16ClN7O2S2
- Masse moléculaire:558.03
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SHMT2-IN-1
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Activité biologique
Description
IC50 & Target
[1]|
SHMT2 1.21 μM (IC50) |
Human SHMT1 1.83 μM (IC50) |
In Vitro
SHMT2-IN-1 (0.1-10 μM, 24 h) exhibits potent antiproliferative activity against esophageal cancer cells KYSE-450 and KYSE-70 with IC50 values of 1.62 μM and 1.18 μM respectively[1].
SHMT2-IN-1 (2.5-10 μM, 24 h) dose-dependently inhibits the migration and invasion of KYSE-450 and KYSE-70 cells[1].
SHMT2-IN-1 (2.5-7.5 μM, 24-72 h) induces apoptosis, ROS production and cause G2/M phase arrest in KYSE-450 and KYSE-70 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-450 and KYSE-70 cells
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Concentration:2.5, 5 and 7.5 μM
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Incubation Time:72 h
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Result:Increased apoptotic cells.
Upregulated Bax expression and downregulated Bcl-2, Pro-Caspase 3 and Pro-Caspase 9 expression.
Chemical Information
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Appearance Solid
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Masse moléculaire 558.03
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Formule C26H16ClN7O2S2
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Color White to off-white
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SMILES
N#CC1=C(N=C(N=C1C2=CC=C(C=C2)Cl)SCC3=CC=C(C=C3)C(O)=O)SC4=NN=NN4C5=CC=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (179.20 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 2.5 mg/mL (4.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.7920 mL | 8.9601 mL | 17.9202 mL | 44.8005 mL |
| 5 mM | 0.3584 mL | 1.7920 mL | 3.5840 mL | 8.9601 mL | |
| 10 mM | 0.1792 mL | 0.8960 mL | 1.7920 mL | 4.4800 mL | |
| 15 mM | 0.1195 mL | 0.5973 mL | 1.1947 mL | 2.9867 mL | |
| 20 mM | 0.0896 mL | 0.4480 mL | 0.8960 mL | 2.2400 mL | |
| 25 mM | 0.0717 mL | 0.3584 mL | 0.7168 mL | 1.7920 mL | |
| 30 mM | 0.0597 mL | 0.2987 mL | 0.5973 mL | 1.4933 mL | |
| 40 mM | 0.0448 mL | 0.2240 mL | 0.4480 mL | 1.1200 mL | |
| 50 mM | 0.0358 mL | 0.1792 mL | 0.3584 mL | 0.8960 mL | |
| 60 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL | |
| 80 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5600 mL | |
| 100 mM | 0.0179 mL | 0.0896 mL | 0.1792 mL | 0.4480 mL |
SHMT2-IN-1 Related Classifications
HY-178432 Related Classifications
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