NSC-370284
Based on 1 publication(s) in Google Scholar
NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.
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- Purity: 99.27%
- CAS No.: 116409-29-1
- 화학식: C21H25NO6
- 분자량:387.43
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) NSC-370284
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Biological Activity
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STAT3 |
STAT5 |
TET1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-87MG ATCC | IC50 |
24.2 μM
Compound: NC124, NSC 370284
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Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32830969] |
NSC-370284 (0-500 nM; 24 h or 48 h) inhibits the viability of MONOMAC-6, THP-1, KOCL-48 and KASUMI-1 acute myeloid leukemia (AML) cells via targeting STAT3/5. NSC-370284 significantly down-regulates the level of TET1 transcription[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AML cell lines including MONOMAC-6, THP-1, KOCL-48, and KASUMI-1.
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Concentration:0, 25, 50, 200 or 500 nM.
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Incubation Time:24 h or 48 h.
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Result:Showed inhibitory for AML cells viability and TET1 transcription.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (CD45.2) and B6.SJL (CD45.1) mice[1].
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Dosage:2.5 mg/kg.
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Administration:Intraperitoneal injection, once daily, for 10 days.
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Result:Significantly inhibited MLL-AF9 induced AML in secondary bone marrow transplantation (BMT) recipient mice.
Chemical Information
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CAS No. 116409-29-1
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Appearance Solid
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분자량 387.43
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화학식 C21H25NO6
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Color Off-white to light yellow
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SMILES
OC1=C(C(N2CCCC2)C3=CC(OC)=C(OC)C(OC)=C3)C=C(OCO4)C4=C1
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
Mutant huntingtin disrupts TET1 transcription and alters DNA methylation in a Huntington's disease knock-in pig model. [Abstract]2026 Jun 19;45(7):117584. PMID: 42322611
용액&용해도
DMSO : 100 mg/mL (258.11 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 (6.45 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 (6.45 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.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 | 2.5811 mL | 12.9056 mL | 25.8111 mL | 64.5278 mL |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | 12.9056 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL | 6.4528 mL | |
| 15 mM | 0.1721 mL | 0.8604 mL | 1.7207 mL | 4.3019 mL | |
| 20 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2264 mL | |
| 25 mM | 0.1032 mL | 0.5162 mL | 1.0324 mL | 2.5811 mL | |
| 30 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1509 mL | |
| 40 mM | 0.0645 mL | 0.3226 mL | 0.6453 mL | 1.6132 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2906 mL | |
| 60 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8066 mL | |
| 100 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6453 mL |