NSC 617145
Based on 4 publication(s) in Google Scholar
NSC 617145 is a selective werner syndrome helicase (WRN) helicase inhibitor with an IC50 value of 230 nM. NSC 617145 inhibits WRN ATPase, and induces double-strand breaks (DSB) and chromosomal abnormalities. NSC 617145 shows selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases.
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- Pureza : 99.53%
- No. CAS: 203115-63-3
- Fòrmula: C13H10Cl4N2O4
- Peso molecular:400.04
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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) NSC 617145
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Actividad biológica
Descripciòn
IC50 & Target
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Helicase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.4 μM
Compound: NSC 617145
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Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
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[PMID: 38442524] |
| HEK-293T | IC50 |
3.1 μM
Compound: NSC 617145
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Antiproliferative activity against HEK293T cells incubated for 48 hrs by MTT assay
Antiproliferative activity against HEK293T cells incubated for 48 hrs by MTT assay
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[PMID: 38442524] |
| HeLa | IC50 |
2.7 μM
Compound: NSC 617145
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Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
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[PMID: 38442524] |
| K562 | IC50 |
1.8 μM
Compound: NSC 617145
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Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
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[PMID: 38442524] |
| PC-3 | IC50 |
6.8 μM
Compound: NSC 617145
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Antiproliferative activity against human PC-3 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells incubated for 48 hrs by MTT assay
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[PMID: 38442524] |
In Vitro
NSC 617145 (0.75-3 μM; 24-72 hours) shows maximal inhibition of proliferation (98%) at the lowest concentration in a WRN-specific manner in HeLa cells[1].
NSC 617145 (0.75 μM; 6 hours) induces WRN binding to chromatin and proteasomal degradation[1].
In FA-D2-/- cells, NSC 617145 (0.125 μM) acts synergistically with very low concentrations of Mitomycin C to inhibit proliferation in a WRN-dependent manner and induce double-strand breaks (DSB) and chromosomal abnormalities. NSC 617145 exposure results in enhanced accumulation of DNA-PKcs pS2056 foci and Rad51 foci in Mitomycin C-treated FA-deficient cells, suggesting that WRN helicase inhibition prevents processing of Rad51-mediated recombination products and activates NHEJ[1].
NSC 617145, induces cell cycle arrest and apoptosis in human T-cell leukemia virus type 1 (HTLV-1)-transformed adult T-cell leukemia cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.75 μM, 1 μM, 1.5 μM, 2 μM, 3 μM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Inhibited cell proliferation in a WRN-specific manner.
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Cell Line:HeLa cells
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Concentration:0.75 μM
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Incubation Time:6 hours
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Result:Caused WRN to become degraded by a proteasome-mediated pathway.
Chemical Information
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No. CAS 203115-63-3
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Appearance Solid
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Peso molecular 400.04
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Fòrmula C13H10Cl4N2O4
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Color Light yellow to brown
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SMILES
O=C(C(Cl)=C(Cl)C1=O)N1CC(C)(C)CN2C(C(Cl)=C(Cl)C2=O)=O
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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 1 year -20°C 6 months
Publications (4)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 10 mg/mL (25.00 mM; ultrasonic and warming and heat to 60°C; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
In Vivo Dissolution Calculator
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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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 (277 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
[1]. Monika Aggarwal, et al. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway. Cancer Res. 2013 Sep 1;73(17):5497-507. [Content Brief]
[2]. R Moles, et al. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells. J Hematol Oncol. 2016 Nov 9;9(1):121. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4997 mL | 12.4987 mL | 24.9975 mL | 62.4937 mL |
| 5 mM | 0.4999 mL | 2.4997 mL | 4.9995 mL | 12.4987 mL | |
| 10 mM | 0.2500 mL | 1.2499 mL | 2.4997 mL | 6.2494 mL | |
| 15 mM | 0.1666 mL | 0.8332 mL | 1.6665 mL | 4.1662 mL | |
| 20 mM | 0.1250 mL | 0.6249 mL | 1.2499 mL | 3.1247 mL |
NSC 617145 Related Classifications
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