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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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: 99.38%
- CAS 番号: 2770263-77-7
- 分子式: C36H34N8O8
- 分子量:706.70
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
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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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Anti-Aging Compound Library
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Oxygen Sensing Compound Library
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Anti-Breast Cancer Compound Library
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Anti-Pancreatic Cancer Compound Library
HY-L077
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PROTAC Library
HY-L151
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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
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Lactylation Compound Library
HY-L249
生物活性
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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.
化学情報
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CAS 番号 2770263-77-7
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性状 Solid
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分子量 706.70
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分子式 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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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
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 (276 KB)
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SDS (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 1.4150 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 |
SZUH280 関連分類
HY-152147 関連分類
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