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MedKoo Cat#: 562768 | Name: IOX1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

IOX1 is a cell-penetrating broad-spectrum 2-oxoglutarate oxygenase inhibitor.

Chemical Structure

IOX1
IOX1
CAS#5852-78-8

Theoretical Analysis

MedKoo Cat#: 562768

Name: IOX1

CAS#: 5852-78-8

Chemical Formula: C10H7NO3

Exact Mass: 189.0426

Molecular Weight: 189.17

Elemental Analysis: C, 63.49; H, 3.73; N, 7.40; O, 25.37

Price and Availability

Size Price Availability Quantity
100mg USD 350.00 2 Weeks
250mg USD 650.00 2 Weeks
500mg USD 950.00 2 Weeks
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Related CAS #
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Synonym
IOX1; IOX-1; IOX 1;
IUPAC/Chemical Name
8-Hydroxyquinoline-5-carboxylic acid
InChi Key
JGRPKOGHYBAVMW-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H7NO3/c12-8-4-3-7(10(13)14)6-2-1-5-11-9(6)8/h1-5,12H,(H,13,14)
SMILES Code
O=C(C1=C2C=CC=NC2=C(O)C=C1)O
Appearance
Solid powder
Purity
>97% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
In vitro activity:
IOX1 significantly reduced the secretion of TNF-α, IL-1β, IL-6, IL-12p70 and IL-10 induced by LPS (Fig. 1C). The expression of surface molecules, such as CD80, CD86, MHC-I and MHC-II, induced by LPS was also significantly reduced (Fig. 1D). These results indicate that IOX1 can effectively regulate the immune activity of bone marrow DCs induced by LPS. Reference: Sci Rep. 2021 Feb 3;11(1):2942. https://pubmed.ncbi.nlm.nih.gov/33536477/
In vivo activity:
Remarkably, IOX1 treatment reduced the psoriasiform lesions compared to that in calcibeta-treated mice (Figure 1C). Additionally, redness, scaling, and thickness of skin lesions reduced significantly (P < 0.001, P < 0.05, P < 0.01, and P < 0.01 respectively) in the IOX1-treated group (10 mg/kg), as indicated by the decreased PASI score (Figure 1D and E). These data demonstrate the efficacy of IOX1 in alleviating the clinical symptoms of psoriasis. Reference: Heliyon. 2021 Nov 19;7(11):e08433. https://pubmed.ncbi.nlm.nih.gov/34877426/
Solvent mg/mL mM
Solubility
DMSO:PBS (pH 7.2) (1:1) 0.5 2.64
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 189.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Lee SJ, You JS, Gharbi A, Kim YJ, Lee MS, Kim DH, Lee KW, Jung ID, Park YM. IOX1 activity as sepsis therapy and an antibiotic against multidrug-resistant bacteria. Sci Rep. 2021 Feb 3;11(1):2942. doi: 10.1038/s41598-021-82377-z. PMID: 33536477; PMCID: PMC7858575. 2. Tian T, Xie R, Ding K, Han B, Yang Q, Yang X. IOX1 protects from TGF-β induced fibrosis in LX-2 cells via the regulation of extracellular matrix protein expression. Exp Ther Med. 2021 Mar;21(3):180. doi: 10.3892/etm.2021.9611. Epub 2021 Jan 5. PMID: 33488789; PMCID: PMC7812578. 3. Shin JE, Lee SJ, Gharbi A, Jung ID, Park YM. IOX1 impedes host inflammation in imiquimod-triggered psoriasis. Heliyon. 2021 Nov 19;7(11):e08433. doi: 10.1016/j.heliyon.2021.e08433. PMID: 34877426; PMCID: PMC8632842. 4. Hoyle RG, Wang H, Cen Y, Zhang Y, Li J. IOX1 Suppresses Wnt Target Gene Transcription and Colorectal Cancer Tumorigenesis through Inhibition of KDM3 Histone Demethylases. Mol Cancer Ther. 2021 Jan;20(1):191-202. doi: 10.1158/1535-7163.MCT-20-0328. Epub 2020 Nov 17. PMID: 33203729; PMCID: PMC7790990.
In vitro protocol:
1. Lee SJ, You JS, Gharbi A, Kim YJ, Lee MS, Kim DH, Lee KW, Jung ID, Park YM. IOX1 activity as sepsis therapy and an antibiotic against multidrug-resistant bacteria. Sci Rep. 2021 Feb 3;11(1):2942. doi: 10.1038/s41598-021-82377-z. PMID: 33536477; PMCID: PMC7858575. 2. Tian T, Xie R, Ding K, Han B, Yang Q, Yang X. IOX1 protects from TGF-β induced fibrosis in LX-2 cells via the regulation of extracellular matrix protein expression. Exp Ther Med. 2021 Mar;21(3):180. doi: 10.3892/etm.2021.9611. Epub 2021 Jan 5. PMID: 33488789; PMCID: PMC7812578.
In vivo protocol:
1. Shin JE, Lee SJ, Gharbi A, Jung ID, Park YM. IOX1 impedes host inflammation in imiquimod-triggered psoriasis. Heliyon. 2021 Nov 19;7(11):e08433. doi: 10.1016/j.heliyon.2021.e08433. PMID: 34877426; PMCID: PMC8632842. 2. Hoyle RG, Wang H, Cen Y, Zhang Y, Li J. IOX1 Suppresses Wnt Target Gene Transcription and Colorectal Cancer Tumorigenesis through Inhibition of KDM3 Histone Demethylases. Mol Cancer Ther. 2021 Jan;20(1):191-202. doi: 10.1158/1535-7163.MCT-20-0328. Epub 2020 Nov 17. PMID: 33203729; PMCID: PMC7790990.
1: Mettananda S, Fisher CA, Sloane-Stanley JA, Taylor S, Oppermann U, Gibbons RJ, Higgs DR. Selective silencing of α-globin by the histone demethylase inhibitor IOX1: a potentially new pathway for treatment of β-thalassemia. Haematologica. 2017 Mar;102(3):e80-e84. doi: 10.3324/haematol.2016.155655. Epub 2016 Nov 3. PubMed PMID: 27810991; PubMed Central PMCID: PMC5394973. 2: Hu Q, Chen J, Zhang J, Xu C, Yang S, Jiang H. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins. Int J Mol Med. 2016 Jan;37(1):189-96. doi: 10.3892/ijmm.2015.2393. Epub 2015 Oct 27. PubMed PMID: 26530537. 3: Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC, Mott BT, McCullagh JS, Maloney DJ, Schofield CJ, Kawamura A. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71. doi: 10.1002/cmdc.201300428. Epub 2014 Feb 6. PubMed PMID: 24504543; PubMed Central PMCID: PMC4503230. 4: Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JBL, King ONF, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, Lejeune C, Rydzik AM, Rose NR, Bagg EA, McDonough MA, Krojer T, Yue WW, Ng SS, Olsen L, Brennan PE, Oppermann U, Muller-Knapp S, Klose RJ, Ratcliffe PJ, Schofield CJ, Kawamura A. 5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation. Chem Sci. 2013 Aug 1;4(8):3110-3117. doi: 10.1039/C3SC51122G. PubMed PMID: 26682036; PubMed Central PMCID: PMC4678600.