WS6
Based on 1 Customer Validation
WS6 is an IkB kinase and EBP1 inhibitor, with IC50 values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats[1][2][4].
For research use only. We do not sell to patients.
- Purity: 99.30%
- CAS No.: 1421227-53-3
- Formula: C29H31F3N6O3
- Molecular Weight:568.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
All EGFR Isoforms
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Biological Activity
EBP1, IkB[1].
WS6 (1 μM, 48 h) stimulates the proliferation of alpha and beta cells in human pancreatic islets while maintaining cell viability and beta cell differentiation phenotype[1]. WS6 (0-30 μM, 72 h) reduces MYCN protein stability and neuroblastoma tumorigenicity by inhibiting PA2G4 and MYCN protein binding[3]. WS6 (0-1 μM, 72 h) overcomes drug resistance and kills FLT3-ITD AML primitive cells by targeting FLT3-ITD driven kinase in acute myeloid leukemia (AML)[4]. WS6 (0.1, 0.5 μM, 15 min) promotes cell proliferation in the cochlea of neonatal mice by activating ERBB2 phosphorylation and PI3K activity, and enhancing EGFR family signaling[5]. WS6 exhibits better pharmacokinetic characteristics and binding strength with acetylcholinesterase and neurotrophic factors in computer simulations, thus having the potential to treat Alzheimer's disease[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human pancreatic beta and alpha cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Resulted in insulin expression similar to that of the control group islets.
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Cell Line:Kelly and SK-N-BE (2) - C human neuroblastoma tumor cell lines
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Concentration:0-30 μM
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Incubation Time:2 weeks
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Result:Reduced the number and size of colonies in Kelly and SK-N-BE (2) - C cells.
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Cell Line:FLT3-ITD AML (MV4-11 and MOLM13), FLT3-wt AML cell (U937 and HL60), CML (K562), T-ALL (Jurkat), lung adenocarcinoma cell (A549)
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Concentration:0-1 μM
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Incubation Time:72 h
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Result:Exhibits significant cytotoxicity towards FLT3-ITD AML (MV4-11 and MOLM13) and CML (K562) cell lines, with IC50 values of 0.24nM, 0.21nM, and 40.48nM, respectively.
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Cell Line:MCF-7 cell
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Concentration:0.1、0.5 μM
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Incubation Time:15 min
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Result:Increased p-ERBB2 protein expression in breast cancer cell line MCF-7.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild type male Sprague Dawley rat model of chronic unpredictable mild stress (CUMS) induced depression[2].
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Dosage:2.2 mg/kg
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Administration:Intraperitoneal injection (i.p.); once a day; 28 days
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Result:Reversed the reduction of neurogenesis, GABAergic neurons, dendritic complexity, spinal density, and synaptic plasticity associated protein 95 (PSD95) by CUMS.
Chemical Information
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CAS No. 1421227-53-3
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Appearance Solid
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Molecular Weight 568.59
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Formula C29H31F3N6O3
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Color White to light yellow
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SMILES
O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)CC3=CC=C(OC4=NC=NC(NC(C5CC5)=O)=C4)C=C3
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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 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (175.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.5 mg/mL (4.40 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.40 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Boerner BP, George NM, Mir SU, Sarvetnick NE. WS6 induces both alpha and beta cell proliferation without affecting differentiation or viability. Endocr J. 2015;62(4):379-86. [Content Brief]
[2]. Zhang H, et al. WS6 Induces Adult Hippocampal Neurogenesis in Correlation to its Antidepressant Effect on the Alleviation of Depressive-like Behaviors of Rats. Neuroscience. 2021 Oct 1;473:119-129. [Content Brief]
[3]. Massudi H, et al. Inhibitors of the Oncogenic PA2G4-MYCN Protein-Protein Interface. Cancers (Basel). 2023 Mar 17;15(6):1822. [Content Brief]
[4]. Bregante J, et al. Efficacy and Synergy of Small Molecule Inhibitors Targeting FLT3-ITD+ Acute Myeloid Leukemia. Cancers (Basel). 2021 Dec 8;13(24):6181. [Content Brief]
[5]. Zhang J, et al. ERBB2 signaling drives supporting cell proliferation in vitro and apparent supernumerary hair cell formation in vivo in the neonatal mouse cochlea. Eur J Neurosci. 2018 Nov;48(10):3299-3316. [Content Brief]
[6]. Firdoos S, et al. In silico identification of novel stilbenes analogs for potential multi-targeted drugs against Alzheimer's disease. J Mol Model. 2023 Jun 14;29(7):209. [Content Brief]
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 | 1.7587 mL | 8.7937 mL | 17.5874 mL | 43.9684 mL |
| 5 mM | 0.3517 mL | 1.7587 mL | 3.5175 mL | 8.7937 mL | |
| 10 mM | 0.1759 mL | 0.8794 mL | 1.7587 mL | 4.3968 mL | |
| 15 mM | 0.1172 mL | 0.5862 mL | 1.1725 mL | 2.9312 mL | |
| 20 mM | 0.0879 mL | 0.4397 mL | 0.8794 mL | 2.1984 mL | |
| 25 mM | 0.0703 mL | 0.3517 mL | 0.7035 mL | 1.7587 mL | |
| 30 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4656 mL | |
| 40 mM | 0.0440 mL | 0.2198 mL | 0.4397 mL | 1.0992 mL | |
| 50 mM | 0.0352 mL | 0.1759 mL | 0.3517 mL | 0.8794 mL | |
| 60 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 80 mM | 0.0220 mL | 0.1099 mL | 0.2198 mL | 0.5496 mL | |
| 100 mM | 0.0176 mL | 0.0879 mL | 0.1759 mL | 0.4397 mL |