SZUH280
Based on 1 Customer Validation
SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization.
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- Pureza: 99.38%
- No. CAS: 2770263-77-7
- Fòrmula: C36H34N8O8
- Peso molecular:706.70
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Almacenamiento: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
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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HDAC8 0.58 μM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
9.55 μM
Compound: D10
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Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 37607440] |
| A549 | IC50 |
6.04 μM
Compound: 16e
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method
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[PMID: 36516047] |
| A549 | IC50 |
9.55 μM
Compound: 16e
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method
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[PMID: 36516047] |
HDAC8 degradation induced by SZUH280 (5 μM; 20 h) is mediated by the CRBN E3 ubiquitin ligase[1].
SZUH280 (0.1-10 μM; 20 h) can regulate the oncogenic protein expression and suppress cancer metastasis, potentially improving the efficacy of chemotherapy in various types of cancers[1].
SZUH280 (0-20 μM; 72 h) inhibits A549 cell proliferation in a concentration-dependent manner and shows stronger antiproliferative effect with irradiation[1].
SZUH280 (0-20 μM; 72 h) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells[1].
SZUH280 (5 μM; 24 h) hampers DNA damage repair in cancer cells when in combination with irradiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, HCT116, HeLa and MDA-MB-231 cells
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Concentration:0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:20 h
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Result:Efficiently induced HDAC8 degradation in a concentration-dependent manner in A549, HCT116 and HeLa cells. Reduced the IKZF1 protein levels to a lesser extent at 10 μM in A549 cells. Decreased PGM1 expression during glucose deprivation conditions in A549 cells. Decreased SMAD3 and HDAC8 protein levels in MDA-MB-231 cells.
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Cell Line:A549 cells
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Concentration:2.5, 5, 10 and 20 μM
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Incubation Time:72 h
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Result:Effectively inhibited cell proliferation in a concentration-dependent manner with an IC50 of 9.55 μM. Co-treatment with irradiation exhibited an even stronger antiproliferative effect (with an IC50 value of about 6.04 μM).
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Cell Line:A549 cells
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:72 h
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Result:Effectively induced apoptosis in a dose-dependent manner.
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Cell Line:A549 cells
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:72 h
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Result:Induced cell cycle arrest at the G2/M phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice (severe combined immunodeficient mice), A549 model[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection, every 5 days for 6 weeks
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Result:Exhibited a significantly greater anti-lung cancer activity in vivo than the control group. When in combination with 3 Gy irradiation, achieved a much stronger antitumor activity.
Chemical Information
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No. CAS 2770263-77-7
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Appearance Solid
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Peso molecular 706.70
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Fòrmula C36H34N8O8
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C2C(N(C=C2)CC3=CC=C(C=C3)OCCOCCN4C=C(N=N4)CNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=C1)NO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 116.67 mg/mL (165.09 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)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 1.4150 mL | 7.0751 mL | 14.1503 mL | 35.3757 mL |
| 5 mM | 0.2830 mL | 1.4150 mL | 2.8301 mL | 7.0751 mL | |
| 10 mM | 0.1415 mL | 0.7075 mL | 1.4150 mL | 3.5376 mL | |
| 15 mM | 0.0943 mL | 0.4717 mL | 0.9434 mL | 2.3584 mL | |
| 20 mM | 0.0708 mL | 0.3538 mL | 0.7075 mL | 1.7688 mL | |
| 25 mM | 0.0566 mL | 0.2830 mL | 0.5660 mL | 1.4150 mL | |
| 30 mM | 0.0472 mL | 0.2358 mL | 0.4717 mL | 1.1792 mL | |
| 40 mM | 0.0354 mL | 0.1769 mL | 0.3538 mL | 0.8844 mL | |
| 50 mM | 0.0283 mL | 0.1415 mL | 0.2830 mL | 0.7075 mL | |
| 60 mM | 0.0236 mL | 0.1179 mL | 0.2358 mL | 0.5896 mL | |
| 80 mM | 0.0177 mL | 0.0884 mL | 0.1769 mL | 0.4422 mL | |
| 100 mM | 0.0142 mL | 0.0708 mL | 0.1415 mL | 0.3538 mL |
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