1. Cell Cycle/DNA Damage Stem Cell/Wnt Epigenetics
  2. Casein Kinase HDAC
  3. 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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IOR-160

IOR-160 Chemical Structure

CAS No. : 2421119-78-8

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Description

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[1].

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
Cell Line Type Value Description References
A549 IC50
104.73 μM
Compound: 15c
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
[PMID: 32435375]
LNCaP IC50
16.31 μM
Compound: 15c
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
[PMID: 32435375]
MCF7 IC50
52.48 μM
Compound: 15c
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
[PMID: 32435375]
PC-3 IC50
40.42 μM
Compound: 15c
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
[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

IOR-160 (1.0 mg in 100 μL of PBS, injected intratumorally, three times a week, 26 days) reduces tumor growth through dual CK2/HDAC inhibition in nonobese diabetic (NOD) scid gamma mice bearing MDA-MB-231 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA-MB-231 cells (3 × 106) xenograft NOD scid gamma mice (8-week-old) Model[1]
Dosage: 1.0 mg in 100 μL of PBS
Administration: injected intratumorally, three times a week, 26 days
Result: Reduced tumor growth.
Reduced pAKT levels and increased acetylated α-tubulin.
Molecular Weight

510.46

Formula

C23H25F3N4O6

CAS No.
SMILES

O=C(NO)CCCCCCCNC1=NC2=C(C=CC(C(O)=O)=C2)C3=CN=CC=C31.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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IOR-160
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HY-176561
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