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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.00%
- 分子式: C23H29N3O5S3
- 分子量:523.69
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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
化学情報
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性状 Solid
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分子量 523.69
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 |