NMS-859 |
| Katalog-Nr.GC32874 |
NMS-859 ist ein potenter, kovalenter VCP (p97)-Inhibitor mit IC50-Werten von 0,37 und 0,36 μM fÜr Wildtyp-VCP in Gegenwart von 60 μM bzw. 1 mM ATP in Zellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1449236-96-7
Sample solution is provided at 25 µL, 10mM.
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NMS-859 is a potent, covalent VCP (p97) inhibitor, with IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively.
NMS-859 is a potent VCP inhibitor, with IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively. NMS-859 shows very weak inhibitory activity against VCPC522T. NMS-859 also suppresses the proliferation of cells, with IC50s of 3.5 μM and 3.0 μM in HCT116 and HeLa cell lines, respectively[1].
[1]. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol. 2013 Sep;9(9):548-56.
Cell experiment: | Cells are seeded at 1,600 cells per well in 384-well white clear-bottom plates. Twenty-four hours after seeding, cells are treated with NMS-859 (eight dilution points, in duplicate) and incubated for an additional 72 h at 37°C under a 5% CO2 atmosphere. Cells are then lysed, and the ATP content in each well is determined using a thermostable firefly luciferase-based assay as a measure of cell viability. IC50 values are calculated using the percentage of growth of treated cells versus the untreated control[1]. |
References: [1]. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol. 2013 Sep;9(9):548-56. | |
| Cas No. | 1449236-96-7 | SDF | |
| Canonical SMILES | O=S1(C2=CC=CC=C2C(NC3=CC(NC(CCl)=O)=CC=C3)=N1)=O | ||
| Formula | C15H12ClN3O3S | M.Wt | 349.79 |
| Löslichkeit | DMSO : ≥ 42 mg/mL (120.07 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8589 mL | 14.2943 mL | 28.5886 mL |
| 5 mM | 0.5718 mL | 2.8589 mL | 5.7177 mL |
| 10 mM | 0.2859 mL | 1.4294 mL | 2.8589 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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