Structure of IOX1
CAS No.: 5852-78-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
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 | PMC11515915 |
MFC cells | 5 μM | 48 h | IOX1 significantly increased the expression of IFN-stimulated genes (ISGs), such as CXCL10, ISG15 and IFNB1 | PMC11515915 |
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. | PMC5897363 |
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. | PMC5897363 |
CT26 cells | 5, 25, 50 μM | 24 h | Inhibited P-gp expression and enhanced DOX cytotoxicity | PMC8065121 |
HCT116 cells | 5, 25, 50 μM | 24 h | Inhibited P-gp expression and enhanced DOX cytotoxicity | PMC8065121 |
CT26 cells | 25 μM | 4 h | Enhanced DOX-induced immunogenic cell death (ICD) | PMC8065121 |
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. | PMC5309163 |
ESCC cells | 50 µM | 24 h | IOX1 increased H3K9me2 levels and slightly altered H3K27me3 levels, while decreasing the protein expression of KDM3A and KDM6B. | PMC7736883 |
ESCC cells | 20 µM | IOX1 decreased the survival fraction of all ESCC cells and increased sensitivity to radiotherapy. | PMC7736883 | |
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 | PMC9646865 |
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 | PMC9646865 |
A549 | 40 μM | 48 h | IOX1 significantly enhanced the radiosensitivity of A549 cells, significantly increasing γirradiation-induced apoptosis. | PMC10716120 |
H1299 | 40 μM | 48 h | IOX1 significantly enhanced the radiosensitivity of H1299 cells, significantly increasing γirradiation-induced apoptosis. | PMC10716120 |
H1975 | 40 μM | 48 h | IOX1 significantly enhanced the radiosensitivity of H1975 cells, significantly increasing γirradiation-induced apoptosis. | PMC10716120 |
HeLa | 40 μM | 48 h | IOX1 significantly enhanced the radiosensitivity of HeLa cells, significantly increasing γirradiation-induced apoptosis. | PMC10716120 |
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. | PMC9977869 |
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 | PMC11515915 |
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 | PMC8065121 |
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 | PMC9646865 |
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. | PMC10716120 |
Tags: IOX1 | IOX 1 | IOX-1 | Histone Demethylase | 2OG oxygenase inhibitor | JmjC demethylases | KDM4C inhibitor | KDM4E inhibitor | ALKBH5 inhibitor | epigenetic regulation | epigenetic regulation | chromatin remodeling | 5852-78-8
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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