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Chemical Structure| 5852-78-8 Chemical Structure| 5852-78-8

Structure of IOX1
CAS No.: 5852-78-8

Chemical Structure| 5852-78-8

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IOX1 is the broad-spectrum inhibitor of 2OG oxygenases and its IC50 for KDM4A/KDM3A and KDM4C/KDM6B/KDM2A/KDM4E are 0.6/0.1 μM and 0.6 μM/1.6 μM/1.8 μM/2.3 μM.

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Product Details of IOX1

CAS No. :5852-78-8
Formula : C10H7NO3
M.W : 189.17
SMILES Code : O=C(C1=C2C=CC=NC2=C(O)C=C1)O
MDL No. :MFCD18417145
InChI Key :JGRPKOGHYBAVMW-UHFFFAOYSA-N
Pubchem ID :459617

Safety of IOX1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of IOX1

epigenetics

Isoform Comparison

Biological Activity

Target
  • KDM2

    KDM2A, IC50:1.8 μM

  • KDM4

    KDM4E, IC50:2.3 μM

    KDM4C, IC50:0.6 μM

  • KDM6

    KDM6B, IC50:1.6 μM

  • KDM5

    KDM5C, IC50:19 μM

  • KDM3

    KDM3A, IC50:0.1 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
AGS cells 5 μM 48 h IOX1 significantly increased the expression of IFN-stimulated genes (ISGs), such as CXCL10, ISG15 and IFNB1 Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
MFC cells 5 μM 48 h IOX1 significantly increased the expression of IFN-stimulated genes (ISGs), such as CXCL10, ISG15 and IFNB1 Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
Mouse keratinocytes 200 µM 24 h To study the effect of IOX-1 on IL-23A expression, results showed that IOX-1 significantly reduced IL-23A expression. Nat Commun. 2018 Apr 12;9(1):1420.
Human keratinocytes 200 µM 24 h To study the effect of IOX-1 on IL-23A expression, results showed that IOX-1 significantly reduced IL-23A expression. Nat Commun. 2018 Apr 12;9(1):1420.
CT26 cells 5, 25, 50 μM 24 h Inhibited P-gp expression and enhanced DOX cytotoxicity Nat Commun. 2021 Apr 23;12(1):2425.
HCT116 cells 5, 25, 50 μM 24 h Inhibited P-gp expression and enhanced DOX cytotoxicity Nat Commun. 2021 Apr 23;12(1):2425.
CT26 cells 25 μM 4 h Enhanced DOX-induced immunogenic cell death (ICD) Nat Commun. 2021 Apr 23;12(1):2425.
HEK293 cells 100 μM 24 h To evaluate the inhibitory effect of IOX1 on histone demethylation, results showed that IOX1 treatment significantly increased the levels of me3Lys and me2Lys. Anal Chem. 2017 Jan 17;89(2):1299-1306.
ESCC cells 50 µM 24 h IOX1 increased H3K9me2 levels and slightly altered H3K27me3 levels, while decreasing the protein expression of KDM3A and KDM6B. Cell Death Dis. 2020 Dec 14;11(12):1068.
ESCC cells 20 µM IOX1 decreased the survival fraction of all ESCC cells and increased sensitivity to radiotherapy. Cell Death Dis. 2020 Dec 14;11(12):1068.
Murine CD4+ T cells 10 μM and 20 μM 72 h To evaluate the effect of IOX1 on Th1 and Th17 cell differentiation, results showed that IOX1 significantly suppressed IL-17 expression but had less effect on IFN-γ expression EBioMedicine. 2022 Dec;86:104333.
Human peripheral blood CD4+ T cells 25 μM and 100 μM 5 days To evaluate the effect of IOX1 on human CD4+ T cell proliferation and differentiation, results showed that IOX1 dose-dependently suppressed IFN-γ and IL-17 expression EBioMedicine. 2022 Dec;86:104333.
A549 40 μM 48 h IOX1 significantly enhanced the radiosensitivity of A549 cells, significantly increasing γirradiation-induced apoptosis. Cell Death Dis. 2023 Dec 12;14(12):817.
H1299 40 μM 48 h IOX1 significantly enhanced the radiosensitivity of H1299 cells, significantly increasing γirradiation-induced apoptosis. Cell Death Dis. 2023 Dec 12;14(12):817.
H1975 40 μM 48 h IOX1 significantly enhanced the radiosensitivity of H1975 cells, significantly increasing γirradiation-induced apoptosis. Cell Death Dis. 2023 Dec 12;14(12):817.
HeLa 40 μM 48 h IOX1 significantly enhanced the radiosensitivity of HeLa cells, significantly increasing γirradiation-induced apoptosis. Cell Death Dis. 2023 Dec 12;14(12):817.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Renal ischemia-reperfusion injury model Tail vein injection 10 mg/kg Single administration before surgery IOX1 alleviates renal ischemia-reperfusion injury by increasing m6A methylation and regulating the CCL28/Treg/inflammatory cell axis. Nat Commun. 2023 Mar 1;14(1):1161
Mice Subcutaneous xenograft model in nude mice Intraperitoneal injection 12.5 mg/kg Every 2 days, continued treatment IOX1 significantly suppressed tumor growth, decreased tumor volume, and reduced tumor weight Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
BALB/c mice S.c. CT26 tumour model Intravenous injection 7.5 mg/kg Every 2 days for 3 times IPLD significantly inhibited tumour growth and induced immune memory Nat Commun. 2021 Apr 23;12(1):2425.
B10.RIII mice Experimental autoimmune uveoretinitis (EAU) model Intraperitoneal injection 12.5 mg/kg Twice daily, until peak disease (Day 14) To evaluate the effect of IOX1 on Th17 cell migration and inflammation in the EAU model, results showed that IOX1 significantly reduced the migration of Th17 cells into the site of inflammation and tissue damage EBioMedicine. 2022 Dec;86:104333.
Nude mice A549 xenograft model Injection 10 mg/kg Once a day for 6 days IOX1 significantly suppressed the growth of A549 tumors and enhanced the tumor's sensitivity to radiation. Cell Death Dis. 2023 Dec 12;14(12):817.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.29mL

1.06mL

0.53mL

26.43mL

5.29mL

2.64mL

52.86mL

10.57mL

5.29mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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