WH-4-023
Based on 5 publication(s) in Google Scholar
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 837422-57-8
- Fòrmula: C32H36N6O4
- Peso molecular:568.67
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) WH-4-023
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WB
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RT-PCR
Actividad biológica
IC50: 2 nM (Lck), 6 nM (Src)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | IC50 |
1.9 μM
Compound: 28
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Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells
Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells
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[PMID: 16884310] |
Chemical Information
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No. CAS 837422-57-8
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Appearance Solid
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Peso molecular 568.67
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Fòrmula C32H36N6O4
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Color White to off-white
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SMILES
O=C(OC1=C(C)C=CC=C1C)N(C2=CC=C(OC)C=C2OC)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C3
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Synonyms
Dual LCK/SRC inhibitor
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Mol Cancer
Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. [Abstract]2022 Mar 18;21(1):77. PMID: 35303882
WH-4-023 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
Cells were treated with gefitinib, osimertinib, lapatinib, WH-4-023 or SCH772984 for 48 h, Western blot assay showed the proteins level.
WH-4-023 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
CHIP-qPCR analysis was performed after cells treated with osimertinib, SCH772984, WH-4-023 for 48 h in H1975 cells.
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Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Cell Mol Gastroenterol Hepatol
2021;11(3):683-696. PMID: 33075564 -
J Biol Chem
c-Src regulates δ-secretase activation and truncated Tau production by phosphorylating the E3 ligase Traf6. [Abstract]2023 Dec;299(12):105462. PMID: 37977223 -
Methods Mol Biol
2024:2767:1-18. PMID: 37351840
Solvente y solubilidad
DMSO : 25 mg/mL (43.96 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 0.77 mg/mL (1.35 mM); Clear solution
This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 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.
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.
Protocolo
The Lck HTRF kinase assay involves ATP-dependent phosphorylation of a biotinylated substrate peptide of gastrin in the presence or absence of inhibitor compound. The final concentration of gastrin is 1.2 μM. The final concentration of ATP is 0.5 μM (Km app =0.6±0.1 μM), and the final concentration of Lck (a GST-kinase domain fusion (AA 225−509)) is 250 pM. Buffer conditions are as follows: 50 mM HEPES pH=7.5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl2, 2 mM DTT, 0.05% BSA. The assay is quenched and stopped with 160 μL of detection reagent. Detection reagents are as follows: Buffer made of 50 mM Tris, pH=7.5, 100 mM NaCl, 3 mM EDTA, 0.05% BSA, 0.1% Tween20. Prior to reading, Streptavidin allophycocyanin (SA-APC) is added at a final concentration in the assay of 0.0004 mg/mL, along with europilated anti-phosphotyrosine Ab (Eu-anti-PY) at a final conc of 0.025 nM. The assay plate is read in a Discovery fluorescence plate reader with excitation at 320 nm and emission at 615 and 655 nm[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The purpose of this assay is to test the potency of T cell receptor (TCR; CD3) and CD28 signaling pathway inhibitors in human T cells. T cells are purified from human peripheral blood lymphocytes (hPBL) and preincubated with or without compound prior to stimulation with a combination of an anti-CD3 and an anti-CD28 antibody in 96-well tissue culture plates (1×105 T cells/well). Cells are cultured for ~20 h at 37°C in 5% CO2 and then secreted IL-2 in the supernatants is quantified by cytokine ELISA. The cells remaining in the wells are then pulsed with 3H-thymidine overnight to assess the T cell proliferative response. Cells are harvested onto glass fiber filters and 3H-thymidine incorporation into DNA is analyzed by liquid scintillation counter. For comparison purposes, phorbol myristic acid (PMA) and calcium ionophore are used in combination to induce IL-2 secretion from purified T cells. Potential inhibitor compounds are tested for inhibition of this response as described above for anti-CD3 and -CD28 antibodies. Human whole-blood anti-CD3/CD28-induced IL-2 secretion assays are run in a similar fashion as described above using whole blood from normal volunteers diluted 50% in tissue culture medium prior to stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7585 mL | 8.7924 mL | 17.5849 mL | 43.9622 mL |
| 5 mM | 0.3517 mL | 1.7585 mL | 3.5170 mL | 8.7924 mL | |
| 10 mM | 0.1758 mL | 0.8792 mL | 1.7585 mL | 4.3962 mL | |
| 15 mM | 0.1172 mL | 0.5862 mL | 1.1723 mL | 2.9308 mL | |
| 20 mM | 0.0879 mL | 0.4396 mL | 0.8792 mL | 2.1981 mL | |
| 25 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7585 mL | |
| 30 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4654 mL | |
| 40 mM | 0.0440 mL | 0.2198 mL | 0.4396 mL | 1.0991 mL |
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