Crebinostat
Based on 1 publication(s) in Google Scholar
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice.
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- Pureza: 98.83%
- No. CAS: 1092061-61-4
- Fòrmula: C20H23N3O3
- Peso molecular:353.41
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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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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Crebinostat
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Actividad biológica
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HDAC1 0.7 nM (IC50) |
HDAC2 1.0 nM (IC50) |
HDAC3 2.0 nM (IC50) |
HDAC6 9.3 nM (IC50) |
Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells[1].
Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons[1].
Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse primary neuronal cells (dissociated from E17 embryonic mouse forebrain)
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced robust acetylation of AcH4K12 and AcH3K9 in a dose dependent manner with EC50s of 0.29 μM and 0.18 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (9-10 weeks)[1]
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Dosage:25 mg/kg
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Administration:IP; alternate daily between left and right sides of the abdomen, for 10 days
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Result:Enhanced memory of contextual fear conditioning in mice; induced a trend towards an increase in total hippocampal acetylation of both H4K12 and H3K9.
Chemical Information
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No. CAS 1092061-61-4
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Appearance Solid
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Peso molecular 353.41
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Fòrmula C20H23N3O3
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Color White to off-white
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SMILES
O=C(N/N=C/C1=CC=C(C2=CC=CC=C2)C=C1)CCCCCC(NO)=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
Solvente y solubilidad
DMSO : 100 mg/mL (282.96 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, 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 (7.07 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 (7.07 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.
Pureza y Documentación
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Ficha de datos (270 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
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 | 2.8296 mL | 14.1479 mL | 28.2957 mL | 70.7394 mL |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | 14.1479 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 mL | 7.0739 mL | |
| 15 mM | 0.1886 mL | 0.9432 mL | 1.8864 mL | 4.7160 mL | |
| 20 mM | 0.1415 mL | 0.7074 mL | 1.4148 mL | 3.5370 mL | |
| 25 mM | 0.1132 mL | 0.5659 mL | 1.1318 mL | 2.8296 mL | |
| 30 mM | 0.0943 mL | 0.4716 mL | 0.9432 mL | 2.3580 mL | |
| 40 mM | 0.0707 mL | 0.3537 mL | 0.7074 mL | 1.7685 mL | |
| 50 mM | 0.0566 mL | 0.2830 mL | 0.5659 mL | 1.4148 mL | |
| 60 mM | 0.0472 mL | 0.2358 mL | 0.4716 mL | 1.1790 mL | |
| 80 mM | 0.0354 mL | 0.1768 mL | 0.3537 mL | 0.8842 mL | |
| 100 mM | 0.0283 mL | 0.1415 mL | 0.2830 mL | 0.7074 mL |
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