IOR-160
IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
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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: 2421119-78-8
- 分子式: C23H25F3N4O6
- 分子量:510.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
CK2 1.7 nM (IC50) |
HDAC1 3.3 nM (IC50) |
HDAC2 24 nM (IC50) |
HDAC3 3.9 nM (IC50) |
HDAC6 13 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
104.73 μM
Compound: 15c
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Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay
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[PMID: 32435375] |
| LNCaP | IC50 |
16.31 μM
Compound: 15c
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Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay
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[PMID: 32435375] |
| MCF7 | IC50 |
52.48 μM
Compound: 15c
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Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay
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[PMID: 32435375] |
| PC-3 | IC50 |
40.42 μM
Compound: 15c
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Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay
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[PMID: 32435375] |
体外実験
IOR-160 (0.5 μM) shows high inhibitory for CK2 and HIPK2, with remanent activities of -6 % and 7 %, while showing moderate to low inhibition of DYRK1A, CLK2, Pim-1, Mnk2, DRAK1, and TrkA (from 18% to 65%)[1].
IOR-160 shows less potency for HDAC8, with an IC50 of 2200 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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:MDA-MB-231 cells (3 × 106) xenograft NOD scid gamma mice (8-week-old) Model[1]
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Dosage:1.0 mg in 100 μL of PBS
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Administration:injected intratumorally, three times a week, 26 days
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Result:Reduced tumor growth.
Reduced pAKT levels and increased acetylated α-tubulin.
化学情報
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CAS 番号 2421119-78-8
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分子量 510.46
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分子式 C23H25F3N4O6
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SMILES
O=C(NO)CCCCCCCNC1=NC2=C(C=CC(C(O)=O)=C2)C3=CN=CC=C31.O=C(O)C(F)(F)F
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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)
IOR-160 関連分類
HY-176561 関連分類
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