HDAC6/HSP90-IN-2
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer.
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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。
- CAS 番号: 2803866-22-8
- 分子式: C19H22N2O5
- 分子量:358.39
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
|
HDAC6 106 nM (IC50) |
HDAC1 654.5 nM (IC50) |
HDAC3 1539 nM (IC50) |
HDAC7 1691 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | GI50 |
1.7 μM
Compound: 6e
|
Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated upto 72 hrs by CellTiter96 Aqueous One Solution Cell Proliferation assay
Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated upto 72 hrs by CellTiter96 Aqueous One Solution Cell Proliferation assay
|
[PMID: 35834905] |
体外実験
HDAC6/HSP90-IN-2 (compound 6e) (0.05-2 μM; 24 h) effects HSP90, HDAC6 and signaling pathways regulated by Hsp90 dose-dependently[1]. HDAC6/HSP90-IN-2 (compound 6e) (2 μM; 24 h) promotes the acetylation of HSP90[1]. HDAC6/HSP90-IN-2 (compound 6e) (0-100 μM; 24-72 h) inhibits the growth of H1975 non-small cell lung cancer cells[1]. HDAC6/HSP90-IN-2 (compound 6e) (0-2 μM; 24 h) induces apoptosis of H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 cells
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Concentration:0.05, 0.1, 0.5, 1 and 2 μM
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Incubation Time:24 hours
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Result:Showed inhibitory effect to Hsp90 and HDACs dose-dependently and increased the expression levels of Hsp70 and Hsp90 probably by activates HSF1.
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Cell Line:H1975 cells
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Concentration:2 μM
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Incubation Time:24 hours
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Result:Promoted the acetylation of Hsp90 by inhibiting HDAC6, and increased the acetylation at K294 residue of Hsp90.
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Cell Line:H1975 cells
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Concentration:0, 0.5, 1 and 2 μM
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Incubation Time:24 hours
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Result:Induced early and late apoptosis of H1975 cells dose-dependently.
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Cell Line:H1975 cells
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Concentration:0-100 μM
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Incubation Time:24, 48 and 72 h
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Result:Inhibited the growth of H1975 non-small cell lung cancer cells with a GI50 value of 1.7 μM.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-scid IL2Rgammanull (NSG) mouse with H1975 cells xenograft[1]
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Dosage:25-50 mg/kg
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Administration:Intraperitoneal injection; 25-50 mg/kg for every weekdays; for 6 weeks
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Result:Delayed tumor growth after 2 weeks and reduced the growth rates of tumors in mice.
化学情報
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CAS 番号 2803866-22-8
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分子量 358.39
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分子式 C19H22N2O5
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SMILES
OC1=C(C(C)C)C=C(C(N(C)CC2=CC=C(C=C2)C(NO)=O)=O)C(O)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)