CBP/p300-IN-12
Based on 1 publication(s) in Google Scholar
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.72%
- No. CAS: 2738688-57-6
- Fòrmula: C33H29F4N5O6
- Peso molecular:667.61
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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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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
Publications Citing Use of MedChemExpress (MCE) CBP/p300-IN-12
More
Actividad biológica
Descripciòn
IC50 & Target
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CBP/p300 166 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| DU-145 | EC50 |
1.37 μM
Compound: 2
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Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method
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[PMID: 34055218] |
| LNCaP-Clone-FGC | EC50 |
0.0087 μM
Compound: 2
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Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method
Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method
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[PMID: 34055218] |
In Vitro
CBP/p300-IN-12 (Compound 2) shows antiproliferative effect against androgen receptor (AR)-positive LnCaP-FGC cells (EC50 of 87 nM), while displaying significantly less activity in the AR-negative cell line DU-145 (EC50 of 1.37 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2738688-57-6
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Appearance Solid
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Peso molecular 667.61
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Fòrmula C33H29F4N5O6
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Color Off-white to light yellow
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SMILES
C=CC(NC1=CC=CC(NC(NC2=CC3=C([C@]4(OC(N(CC(N(CC5=CC=C(F)C=C5)[C@@H](C)C(F)(F)F)=O)C4=O)=O)CC3)C=C2)=O)=C1)=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 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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EMBO Rep
Histone modifications and Sp1 promote GPR160 expression in bone cancer pain within rodent models. [Abstract]2024 Dec;25(12):5429-5455. PMID: 39448865
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (374.47 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)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.12 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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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+%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 | 1.4979 mL | 7.4894 mL | 14.9788 mL | 37.4470 mL |
| 5 mM | 0.2996 mL | 1.4979 mL | 2.9958 mL | 7.4894 mL | |
| 10 mM | 0.1498 mL | 0.7489 mL | 1.4979 mL | 3.7447 mL | |
| 15 mM | 0.0999 mL | 0.4993 mL | 0.9986 mL | 2.4965 mL | |
| 20 mM | 0.0749 mL | 0.3745 mL | 0.7489 mL | 1.8724 mL | |
| 25 mM | 0.0599 mL | 0.2996 mL | 0.5992 mL | 1.4979 mL | |
| 30 mM | 0.0499 mL | 0.2496 mL | 0.4993 mL | 1.2482 mL | |
| 40 mM | 0.0374 mL | 0.1872 mL | 0.3745 mL | 0.9362 mL | |
| 50 mM | 0.0300 mL | 0.1498 mL | 0.2996 mL | 0.7489 mL | |
| 60 mM | 0.0250 mL | 0.1248 mL | 0.2496 mL | 0.6241 mL | |
| 80 mM | 0.0187 mL | 0.0936 mL | 0.1872 mL | 0.4681 mL | |
| 100 mM | 0.0150 mL | 0.0749 mL | 0.1498 mL | 0.3745 mL |
CBP/p300-IN-12 Related Classifications
HY-132197 Related Classifications
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