CHI-KAT8i5
Based on 1 Customer Validation
CHI-KAT8i5 is a selective and orally active KAT8 inhibitor with a KD value of 19.72 μM. CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7). CHI-KAT8i5 induces cancer cell apoptosis. CHI-KAT8i5 suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.
For research use only. We do not sell to patients.
- Purity: 98.00%
- Formula: C23H29N3O5S3
- Molecular Weight:523.69
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
KD value of 19.72 μM for KAT8
CHI-KAT8i5 (0-72 h) inhibits cell proliferation of KYSE 30 and KYSE 150 cells with IC50s of 2-3 μΜ[1].
CHI-KAT8i5 (5-15 μM; 48 h) induces cancer cell apoptosis in a dose-dependent manner[1].
CHI-KAT8i5 (5-15 μM; 12 h) represses the NPM1 and PPAT transcript expression in a dose-dependent manner[1].
CHI-KAT8i5 (2-15 μM; 12 h) shows a dose-dependent decrease in H4K16ace and c-Myc upon[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE 30 and KYSE 150 cell lines
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Concentration:5 and 15 μM
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Incubation Time:48 h
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Result:Could induce cancer cell apoptosis in a dose-dependent manner.
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Cell Line:KYSE 30 and KYSE 150 cell lines
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Concentration:5 and 15 μM
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Incubation Time:12 h
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Result:NPM1 and PPAT transcript expression were repressed.
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Cell Line:KYSE 30 and KYSE 150 cell lines
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Concentration:2 μΜ, 4 μΜ, 6 μΜ, 10 μΜ, 15 μΜ
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Incubation Time:12 h
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Result:Observed a dose-dependent decrease in H4K16ace and c-Myc.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-to eight-week-old severe combined immunodeficient (SCID) female mice were subdermally implanted with LEG379 tumor tissue[1].
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Dosage:50 or 200 mg/kg
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Administration:Oral gavage; once a day; 4-6-week
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Result:Significantly suppressed tumor growth in the LEG379 (KAT8 high expression levels) case in a dose-dependent manner.
The cell proliferation marker Ki-67 and c-Myc expression were decreased.
The H4K16ace levels were obviously suppressed
Chemical Information
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Appearance Solid
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Molecular Weight 523.69
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Formula C23H29N3O5S3
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Color White to off-white
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SMILES
O=S(C1=CC=C2N=C(/C=C/C3=CC=C(S(=O)(N(CC)CC)=O)C(O)=C3)SC2=C1)(N(CC)CC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (190.95 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)
Purity & Documentation
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Data Sheet (272 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 1.9095 mL | 9.5476 mL | 19.0953 mL | 47.7382 mL |
| 5 mM | 0.3819 mL | 1.9095 mL | 3.8191 mL | 9.5476 mL | |
| 10 mM | 0.1910 mL | 0.9548 mL | 1.9095 mL | 4.7738 mL | |
| 15 mM | 0.1273 mL | 0.6365 mL | 1.2730 mL | 3.1825 mL | |
| 20 mM | 0.0955 mL | 0.4774 mL | 0.9548 mL | 2.3869 mL | |
| 25 mM | 0.0764 mL | 0.3819 mL | 0.7638 mL | 1.9095 mL | |
| 30 mM | 0.0637 mL | 0.3183 mL | 0.6365 mL | 1.5913 mL | |
| 40 mM | 0.0477 mL | 0.2387 mL | 0.4774 mL | 1.1935 mL | |
| 50 mM | 0.0382 mL | 0.1910 mL | 0.3819 mL | 0.9548 mL | |
| 60 mM | 0.0318 mL | 0.1591 mL | 0.3183 mL | 0.7956 mL | |
| 80 mM | 0.0239 mL | 0.1193 mL | 0.2387 mL | 0.5967 mL | |
| 100 mM | 0.0191 mL | 0.0955 mL | 0.1910 mL | 0.4774 mL |
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