CW-069
Based on 1 publication(s) in Google Scholar
CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
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- Purity: 99.37%
- CAS No.: 1594094-64-0
- 화학식: C23H21IN2O3
- 분자량:500.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) CW-069
MoreAll Kinesin Isoforms
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Biological Activity
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HSET 75 μM (IC50) |
CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM. CW-069 shows statistically significant selectivity over KSP. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC50 of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1594094-64-0
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Appearance Solid
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분자량 500.33
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화학식 C23H21IN2O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(I)C=C1C(O)=O)[C@@H](NCC2=CC=CC=C2)CC3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Leukemia
2024 May;38(5):969-980. PMID: 38519798
용액&용해도
DMSO : ≥ 52 mg/mL (103.93 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: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol
The protocol is optimized for use with full-length, N-terminal, 6His-tagged HSET and KSP, and measured the MT-stimulated activity of the proteins. Inhibition of the Gsp synthetase activity of HSET/KSP is observed spectrophotometrically by coupling the hydrolysis of ATP to oxidation of NADH via pyruvate kinase/lactate dehydrogenase reactions. The assay is initiated by adding purified Gsp synthetase/amidase (12.8 nM) to an assay mixture containing the following components (final concentration): 6 nM protein, 0.07 mg/mL MTs, 1.56 mM glutathione, 10 mM spermidine, 2 mM ATP, 2.7 mM MgCl2, 1 mM phospho(enol)-pyruvate, 0.2 mM NADH, 50 μg/mL lactate dehydrogenase, 100 μg/mL pyruvate kinase, and various concentrations of inhibitor (CW-069) all in 50 mM Na PIPES (pH 6.8) at 37°C. The ADP-Glo detection assay is performed. All compound additions are performed using a multidrop BioMek Nxp. Plates are read using a Pherastar microplate reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NHDF cells, HeLa cells, BT549, MCF-7 and MDA-MB-231 cells are verified by STR genotyping and all tested negative for mycoplasma. Cells are cultured in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C and 5% CO2. All compounds (CW-069) used in the Sulforhodamine B colorimetric (SRB) assay are dissolved in DMSO and diluted in culture medium to a final concentration of 0.2% DMSO. For the SRB assay and live-cell imaging, cells are seeded in 96-well plates at a density of 2,500 cells per well. After 24 hr, the cells are treated with compound (CW-069) for 72 hr, with triplicate wells for each concentration. For the SRB assay, the cells are then fixed with trichloroacetic acid (TCA) and stained with SRB. Fluorescence is quantified using an Infinite 200 PRO plate-reader at a wavelength of 545 nm. Compound (CW-069)-treated wells are compared with solvent control wells and the concentration of compound that resulted in 50% of the solvent-control cell growth is designated as the IC50 concentration, calculated using Graphpad PRISM 6. At least three biological replicates are performed for each assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (280 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
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 | 1.9987 mL | 9.9934 mL | 19.9868 mL | 49.9670 mL |
| 5 mM | 0.3997 mL | 1.9987 mL | 3.9974 mL | 9.9934 mL | |
| 10 mM | 0.1999 mL | 0.9993 mL | 1.9987 mL | 4.9967 mL | |
| 15 mM | 0.1332 mL | 0.6662 mL | 1.3325 mL | 3.3311 mL | |
| 20 mM | 0.0999 mL | 0.4997 mL | 0.9993 mL | 2.4984 mL | |
| 25 mM | 0.0799 mL | 0.3997 mL | 0.7995 mL | 1.9987 mL | |
| 30 mM | 0.0666 mL | 0.3331 mL | 0.6662 mL | 1.6656 mL | |
| 40 mM | 0.0500 mL | 0.2498 mL | 0.4997 mL | 1.2492 mL | |
| 50 mM | 0.0400 mL | 0.1999 mL | 0.3997 mL | 0.9993 mL | |
| 60 mM | 0.0333 mL | 0.1666 mL | 0.3331 mL | 0.8328 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6246 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1999 mL | 0.4997 mL |
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