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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- CAS No.: 2421119-78-8
- Formule: C23H25F3N4O6
- Masse moléculaire:510.46
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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] |
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 2421119-78-8
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Masse moléculaire 510.46
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IOR-160 Related Classifications
HY-176561 Related Classifications
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