HDAC9-IN-1
Based on 1 Customer Validation
HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC50 of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC50 values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.
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- Pureté: 95.13%
- Formule: C27H22N4O3S
- Masse moléculaire:482.55
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HDAC9 40 nM (IC50) |
HDAC4 180 nM (IC50) |
HDAC7 190 nM (IC50) |
HDAC6 970 nM (IC50) |
Caspase-8 |
Caspase-9 |
In Vitro
HDAC9-IN-1 (compound 7g) (5-30 min) potently inhibits HDAC 9 and class IIa HDACs 4 and 7 while showing weak activity against HDAC 6 and no activity against class I HDACs (IC50 values: 40 nM (HDAC9), 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6), >40 μM (class I))[1].
HDAC9-IN-1 (24 h) inhibits viability of cancer cells and normal lung fibroblasts (IC50 values: 3.0 μM (SCC2095), 8.4 μM (MDA-MB-231), 5.8 μM (SCM-1), 8.0 μM (normal lung fibroblasts))[1].
HDAC9-IN-1 (1-10 μM; 24-48 h) induces dose- and time-dependent apoptosis in SCC2095 cells[1].
HDAC9-IN-1 (1-10 μM; 24 h) modulates apoptotic, HDAC substrate, and stress response proteins in SCC2095 cells[1].
HDAC9-IN-1 (2.5-5 μM; 12-24 h) increases ROS generation accompanied by the increased DNA damage in SCC2095 cells in a time-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human oral cancer SCC2095 cells
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Concentration:1 μM, 2.5 μM, 5 μM, 7.5 μM, and 10 μM
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Incubation Time:24 h, 48 h
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Result:Induced apoptosis in a dose- and time-dependent manner: 10 μM for 24 h increased apoptotic cells to 83.6%; 1, 2.5, 5, 7.5, 10 μM for 48 h resulted in apoptosis rates of 29.2%, 35.9%, 44.4%, 78.2%, and 87.1%, respectively.
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Cell Line:SCC2095 cells
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Concentration:1 μM, 2.5 μM, 5 μM, 7.5 μM, and 10 μM
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Incubation Time:24 h
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Result:Down-regulated the levels of pro-caspase 8 and up-regulated the levels of cleaved caspase 9.
The levels of HDAC6 substrates such as acetyl-α-tubulin and Hsp90, and two class IIa HDAC-related proteins including
PPARγ and p21 were increased.
Up-regulated the phosphorylation of p38 in a dose-dependent manner in SCC2095 cells.
Increased the phosphorylation of Histone H2A.X, a DNS damage biomarker.
Chemical Information
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Appearance Solid
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Masse moléculaire 482.55
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Formule C27H22N4O3S
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Color Light brown to brown
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SMILES
N/C(C1=CC2=C(SC3=CC=CC=C3N2CC4=CC=C(C(C5=CC=CC=C5)=C4)C(NO)=O)C=C1)=N\O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (103.62 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)
Pureté et documentation
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Fiche technique (286 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.0723 mL | 10.3616 mL | 20.7232 mL | 51.8081 mL |
| 5 mM | 0.4145 mL | 2.0723 mL | 4.1446 mL | 10.3616 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0723 mL | 5.1808 mL | |
| 15 mM | 0.1382 mL | 0.6908 mL | 1.3815 mL | 3.4539 mL | |
| 20 mM | 0.1036 mL | 0.5181 mL | 1.0362 mL | 2.5904 mL | |
| 25 mM | 0.0829 mL | 0.4145 mL | 0.8289 mL | 2.0723 mL | |
| 30 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7269 mL | |
| 40 mM | 0.0518 mL | 0.2590 mL | 0.5181 mL | 1.2952 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 1.0362 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3454 mL | 0.8635 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2590 mL | 0.6476 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5181 mL |
HDAC9-IN-1 Related Classifications
HY-169259 Related Classifications
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Keywords
- HDAC9-IN-1
- HDAC
- DNA/RNA Synthesis
- Reactive Oxygen Species (ROS)
- Apoptosis
- Caspase
- p38 MAPK
- caspase-related proteins
- HDAC9
- normal lung fibroblasts
- MDA-MB-231
- ROS generation
- class IIa HDACs
- apoptosis
- HDAC4
- breast cancer
- molecular modelling
- HDAC6
- class I HDACs
- SCC2095
- p38
- SCM-1
- class IIa HDAC inhibitor
- HDAC7
- human cancer cells
- gastric cancer
- DNA damage
- oral cancer
- Inhibitor
- inhibitor
- inhibit