KVS0001
Based on 2 publication(s) in Google Scholar
KVS0001 is a selective SMG1 inhibitor. KVS0001 elevates the expression of transcripts and proteins resulting from truncating mutations. KVS0001 increased the presentation of immune-targetable HLA class I-associated peptides from nonsense-mediated decay (NMD)-downregulated proteins on the surface of cancer cells. KVS0001 exerts anti-tumor properties and can be studied in research for NMD-related diseases, including cancer and inherited diseases.
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- Pureza: 99.11%
- No. CAS: 3056394-59-0
- Fòrmula: C27H27ClN8O3S
- Peso molecular:579.07
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KVS0001
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Actividad biológica
KVS0001 (10 nM-1 μM) inhibits SMG1 protein more than any other 246 protein or lipid kinases[1].
KVS0001 (0.2-5 μM) is bioactive in nanomolar range and subverts the NMD-mediated downregulation of truncating mutant transcripts and proteins in NCI-H358 and LS180 cells[1].
KVS0001 causes significant increase in IFN-γ release in NCI-H716_A24 and NCI-H2228 cells in the presence of KVS-BI043 bispecific antibody and T cells, as well as leading to significant killing of the target cancer cells[1].
KVS0001 (5 μM) significantly increases RNA in six of the twelve truncating mutation-containing genes and five of the six expression controlled by NMD genes in murine RENCA (renal cancer) and LLC (lung cancer)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KVS0001 (30 μM/mouse, i.p., 5 d on and 3 d off for 10 d) results in slower tumor growth of BALB/c mice[1].
KVS0001 (30 μM/mouse, i.p., single dose) increases transcript levels in each of six tested endogenous genes with truncating mutations, while having no measureable effects on genes containing heterozygous coding region SNPs in NCI-H358- and LS180-derived xenograft tumors in nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six- to eight-week-old immune compromised M. musculus BALB/cAnNCrl (referred to as BALB/c) and C57BL/6NCrl (referred to as C57BL/6N) mice[1]
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Dosage:30 μM/mouse
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Administration:Intraperitoneal injection (i.p.), daily for 10 d (C57BL/6N), 5 d on and 3 d off for 10 d (BALB/c)
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Result:Resulted in slower tumor growth.
Chemical Information
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No. CAS 3056394-59-0
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Appearance Solid
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Peso molecular 579.07
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Fòrmula C27H27ClN8O3S
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Color Light yellow to yellow
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SMILES
ClC1=C(S(N2CCNCC2)(=O)=O)C=C(NC3=NC=CC(C4=CC(C5=CC=C(NC(NC)=O)C=C5)=NC=C4)=N3)C=C1
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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 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Immunity
2026 May 12;59(5):1398-1421.e20. PMID: 41956098 -
Solvente y solubilidad
DMSO : 100 mg/mL (172.69 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, 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)
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 (4.32 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 (4.32 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.
Pureza y Documentación
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Ficha de datos (272 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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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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7269 mL | 8.6345 mL | 17.2691 mL | 43.1727 mL |
| 5 mM | 0.3454 mL | 1.7269 mL | 3.4538 mL | 8.6345 mL | |
| 10 mM | 0.1727 mL | 0.8635 mL | 1.7269 mL | 4.3173 mL | |
| 15 mM | 0.1151 mL | 0.5756 mL | 1.1513 mL | 2.8782 mL | |
| 20 mM | 0.0863 mL | 0.4317 mL | 0.8635 mL | 2.1586 mL | |
| 25 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7269 mL | |
| 30 mM | 0.0576 mL | 0.2878 mL | 0.5756 mL | 1.4391 mL | |
| 40 mM | 0.0432 mL | 0.2159 mL | 0.4317 mL | 1.0793 mL | |
| 50 mM | 0.0345 mL | 0.1727 mL | 0.3454 mL | 0.8635 mL | |
| 60 mM | 0.0288 mL | 0.1439 mL | 0.2878 mL | 0.7195 mL | |
| 80 mM | 0.0216 mL | 0.1079 mL | 0.2159 mL | 0.5397 mL | |
| 100 mM | 0.0173 mL | 0.0863 mL | 0.1727 mL | 0.4317 mL |
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