L002
Based on 1 Customer Validation
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.44%
- No. CAS: 321695-57-2
- Fòrmula: C15H15NO5S
- Peso molecular:321.35
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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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Actividad biológica
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CBP/p300 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | CC50 |
1.03 μM
Compound: 70
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Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by [3H]-thymidine incorporation assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by [3H]-thymidine incorporation assay
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[PMID: 33045661] |
L002 also has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 μM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500 ng/kg/min) for 4 weeks[3]
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Dosage:20 μg/gm body weight; every 3rd day; 2 weeks
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Administration:Intraperitoneal injection
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Result:Reversed hypertension-induced cardiac fibrosis in mice.
Chemical Information
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No. CAS 321695-57-2
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Appearance Solid
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Peso molecular 321.35
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Fòrmula C15H15NO5S
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Color Light yellow to yellow
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SMILES
O=C1C(C)=C/C(C=C1C)=N\OS(=O)(C2=CC=C(OC)C=C2)=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
Solvente y solubilidad
DMSO : 62.5 mg/mL (194.49 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: ≥ 2.08 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (274 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Rai R, et al. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. [Content Brief]
[2]. Sun XJ, et al. The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol. 2015 May 26;5:108. [Content Brief]
[3]. Rai R, et al. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis.J Cell Mol Med. 2019 Apr;23(4):3026-3031. [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, 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 | 3.1119 mL | 15.5594 mL | 31.1187 mL | 77.7968 mL |
| 5 mM | 0.6224 mL | 3.1119 mL | 6.2237 mL | 15.5594 mL | |
| 10 mM | 0.3112 mL | 1.5559 mL | 3.1119 mL | 7.7797 mL | |
| 15 mM | 0.2075 mL | 1.0373 mL | 2.0746 mL | 5.1865 mL | |
| 20 mM | 0.1556 mL | 0.7780 mL | 1.5559 mL | 3.8898 mL | |
| 25 mM | 0.1245 mL | 0.6224 mL | 1.2447 mL | 3.1119 mL | |
| 30 mM | 0.1037 mL | 0.5186 mL | 1.0373 mL | 2.5932 mL | |
| 40 mM | 0.0778 mL | 0.3890 mL | 0.7780 mL | 1.9449 mL | |
| 50 mM | 0.0622 mL | 0.3112 mL | 0.6224 mL | 1.5559 mL | |
| 60 mM | 0.0519 mL | 0.2593 mL | 0.5186 mL | 1.2966 mL | |
| 80 mM | 0.0389 mL | 0.1945 mL | 0.3890 mL | 0.9725 mL | |
| 100 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7780 mL |
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