CCT251236
Based on 5 publication(s) in Google Scholar
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
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- Pureza: 99.04%
- No. CAS: 1693731-40-6
- Fòrmula: C32H32N4O5
- Peso molecular:552.62
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CCT251236
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Actividad biológica
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HSP72 19 nM (IC50, SK-OV-3 cells) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-OV-3 | GI50 |
1.1 nM
Compound: 26
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Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay
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[PMID: 28004573] |
| SK-OV-3 | GI50 |
2.2 nM
Compound: 26
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Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay
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[PMID: 28004573] |
| SK-OV-3 | GI50 |
2.2 nM
Compound: 1; CCT251236
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Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay
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[PMID: 37017629] |
| WM 266-4 | GI50 |
12 nM
Compound: 26
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Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay
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[PMID: 28004573] |
CCT251236 (0-100 nM; 24hours) displays a desired balance of in vitro properties, while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC50=19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI50 is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay[1]. CCT251236 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72 and HSP27 expression as a concentration manner in SK-OV-3 cells[1]. CCT251236 (0-100 nM; 24 hours), pre-treated with 250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-OV-3 cells
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Concentration:0 nM; 10 nM; 100 nM
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Incubation Time:24 hours
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Result:Inhibited HSP72 and HSP27 expression at the dose of 10 nM.
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Cell Line:SK-OV-3 cells
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Concentration:0 nM; 10 nM; 100 nM and 1000 nM
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Incubation Time:24 hours
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Result:Decreased HSPA1A mRNA level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic mice with SK-OV-3 cells[2]
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Dosage:20 mg/kg; 33 days
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Administration:Oral adminstation
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Result:Was efficacious in SK-OV-3 cell induced-tumor mice model.
Chemical Information
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No. CAS 1693731-40-6
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Appearance Solid
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Peso molecular 552.62
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Fòrmula C32H32N4O5
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Color White to off-white
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SMILES
CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=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 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Proc Natl Acad Sci U S A
2021 Feb 16;118(7):e2014457118. PMID: 33568529 -
Mol Med
Baicalin alleviates chronic obstructive pulmonary disease through regulation of HSP72-mediated JNK pathway. [Abstract]2021 May 30;27(1):53. PMID: 34053448 -
Mol Oncol
Pirin: a potential novel therapeutic target for castration-resistant prostate cancer regulated by miR-455-5p. [Abstract]2019 Feb;13(2):322-337. PMID: 30444038 -
Solvente y solubilidad
DMSO : 100 mg/mL (180.96 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, 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: ≥ 2.5 mg/mL (4.52 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.
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 (276 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
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 | 1.8096 mL | 9.0478 mL | 18.0956 mL | 45.2390 mL |
| 5 mM | 0.3619 mL | 1.8096 mL | 3.6191 mL | 9.0478 mL | |
| 10 mM | 0.1810 mL | 0.9048 mL | 1.8096 mL | 4.5239 mL | |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 mL | |
| 20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2620 mL | |
| 25 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8096 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1310 mL | |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 80 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5655 mL | |
| 100 mM | 0.0181 mL | 0.0905 mL | 0.1810 mL | 0.4524 mL |
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