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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.00%
- Fòrmula: C23H29N3O5S3
- Peso molecular:523.69
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
KD value of 19.72 μM for KAT8
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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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Peso molecular 523.69
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Fòrmula 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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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
Solvente y solubilidad
In Vitro:
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)
Protocolo
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureza y Documentación
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Ficha de datos (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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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 | 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 |
CHI-KAT8i5 Related Classifications
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