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MedKoo Cat#: 401512 | Name: IOX 2
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Description:

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

IOX 2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) (IC50 = 21 nM). IOX 2 displays over 100-fold selectivity for PHD2 over factor inhibiting HIF-1 (FIH-1) and histone demethylases.

Chemical Structure

IOX 2
IOX 2
CAS#931398-72-0

Theoretical Analysis

MedKoo Cat#: 401512

Name: IOX 2

CAS#: 931398-72-0

Chemical Formula: C19H16N2O5

Exact Mass: 352.1059

Molecular Weight: 352.35

Elemental Analysis: C, 64.77; H, 4.58; N, 7.95; O, 22.70

Price and Availability

Size Price Availability Quantity
100mg USD 850.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 3,250.00 2 Weeks
2g USD 4,650.00 2 Weeks
5g USD 6,750.00 2 Weeks
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Related CAS #
No Data
Synonym
IOX2; IOX-2; IOX 2
IUPAC/Chemical Name
N-[[1,2-Dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]glycine
InChi Key
CAOSCCRYLYQBES-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H16N2O5/c22-15(23)10-20-18(25)16-17(24)13-8-4-5-9-14(13)21(19(16)26)11-12-6-2-1-3-7-12/h1-9,24H,10-11H2,(H,20,25)(H,22,23)
SMILES Code
O=C(O)CNC(C1=C(O)C2=C(N(CC3=CC=CC=C3)C1=O)C=CC=C2)=O
Appearance
Solid powder
Purity
>98%
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, not in water
Shelf Life
>5 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:
IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM.
In vitro activity:
In the presence of IOX2, the flagellin-induced rise in intracellular lactate levels was less clear and not statistically significant (p = 0.06 versus IOX2 in medium control). Remarkably, however, IOX2 caused a higher intracellular accumulation of pyruvate regardless of the presence or absence of flagellin (Figure 2B). In accordance, RNA sequencing and GSE analysis indicated that IOX2 significantly impacted the flagellin-induced expression of genes encoding enzymes involved in the core glycolysis pathway (Figure 2C,D). Of interest, IOX2 strongly induced the expression of PKM, the gene encoding pyruvate kinase M, the rate-limiting enzyme that catalyzes the final step of glycolysis, resulting in pyruvate generation, whilst IOX2 did not affect the expression of LDHA, the gene encoding lactate dehydrogenase A, the enzyme responsible for the conversion of pyruvate into lactate (Figure 2D and Figure S2A). Collectively, these results suggest that IOX2 enhances flagellin-induced glycolysis in HBE cells, resulting in the accumulation of intracellular pyruvate. Reference: Cells. 2022 Jan 24;11(3):391. https://pubmed.ncbi.nlm.nih.gov/35159204/
In vivo activity:
Dexmedetomidine treatment notably reduced infarct size, and this effect was partly diminished by IOX2. Dexmedetomidine also reduced the levels of the HIF‐1α, BAX, BNIP3, cleaved caspase‐3 and cleaved PARP‐1 proteins and increased the BCL‐2 protein level and the ratio of BCL‐2 to BAX, while IOX2 treatment partly abolished these effects (Figure 6B). Reference: J Cell Mol Med. 2020 Jan;24(1):850-861. https://pubmed.ncbi.nlm.nih.gov/31680420/
Solvent mg/mL mM
Solubility
DMF 14.0 39.73
DMF:PBS (pH 7.2) (1:1) 0.5 1.42
DMSO 18.1 51.25
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 352.35 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. Ramirez-Moral I, Ferreira BL, Butler JM, van Weeghel M, Otto NA, de Vos AF, Yu X, de Jong MD, Houtkooper RH, van der Poll T. HIF-1α Stabilization in Flagellin-Stimulated Human Bronchial Cells Impairs Barrier Function. Cells. 2022 Jan 24;11(3):391. doi: 10.3390/cells11030391. PMID: 35159204; PMCID: PMC8834373. 2. Jian CB, Yu XE, Gao HD, Chen HA, Jheng RH, Chen CY, Lee HM. Liposomal PHD2 Inhibitors and the Enhanced Efficacy in Stabilizing HIF-1α. Nanomaterials (Basel). 2022 Jan 3;12(1):163. doi: 10.3390/nano12010163. PMID: 35010112; PMCID: PMC8746909. 3. Peng K, Chen WR, Xia F, Liu H, Meng XW, Zhang J, Liu HY, Xia ZY, Ji FH. Dexmedetomidine post-treatment attenuates cardiac ischaemia/reperfusion injury by inhibiting apoptosis through HIF-1α signalling. J Cell Mol Med. 2020 Jan;24(1):850-861. doi: 10.1111/jcmm.14795. Epub 2019 Nov 3. PMID: 31680420; PMCID: PMC6933328.
In vitro protocol:
1. Ramirez-Moral I, Ferreira BL, Butler JM, van Weeghel M, Otto NA, de Vos AF, Yu X, de Jong MD, Houtkooper RH, van der Poll T. HIF-1α Stabilization in Flagellin-Stimulated Human Bronchial Cells Impairs Barrier Function. Cells. 2022 Jan 24;11(3):391. doi: 10.3390/cells11030391. PMID: 35159204; PMCID: PMC8834373. 2. Jian CB, Yu XE, Gao HD, Chen HA, Jheng RH, Chen CY, Lee HM. Liposomal PHD2 Inhibitors and the Enhanced Efficacy in Stabilizing HIF-1α. Nanomaterials (Basel). 2022 Jan 3;12(1):163. doi: 10.3390/nano12010163. PMID: 35010112; PMCID: PMC8746909.
In vivo protocol:
1. Peng K, Chen WR, Xia F, Liu H, Meng XW, Zhang J, Liu HY, Xia ZY, Ji FH. Dexmedetomidine post-treatment attenuates cardiac ischaemia/reperfusion injury by inhibiting apoptosis through HIF-1α signalling. J Cell Mol Med. 2020 Jan;24(1):850-861. doi: 10.1111/jcmm.14795. Epub 2019 Nov 3. PMID: 31680420; PMCID: PMC6933328.
 1: Deppe J, Popp T, Egea V, Steinritz D, Schmidt A, Thiermann H, Weber C, Ries C. Impairment of hypoxia-induced HIF-1α signaling in keratinocytes and fibroblasts by sulfur mustard is counteracted by a selective PHD-2 inhibitor. Arch Toxicol. 2015 Jun 17. [Epub ahead of print] PubMed PMID: 26082309. 2: Egert AM, Klotz JL, McLeod KR, Harmon DL. Development of a methodology to measure the effect of ergot alkaloids on forestomach motility using real-time wireless telemetry. Front Chem. 2014 Oct 13;2:90. doi: 10.3389/fchem.2014.00090. eCollection 2014. PubMed PMID: 25353021; PubMed Central PMCID: PMC4195290. 3: Sen A, Ren S, Lerchenmüller C, Sun J, Weiss N, Most P, Peppel K. MicroRNA-138 regulates hypoxia-induced endothelial cell dysfunction by targeting S100A1. PLoS One. 2013 Nov 11;8(11):e78684. doi: 10.1371/journal.pone.0078684. eCollection 2013. Erratum in: PLoS One. 2013;8(12). doi:10.1371/annotation/53080a85-89cc-4a84-8fd9-0eb0c19cc05d. PLoS One. 2014;9(1). doi:10.1371/annotation/c7bddd8d-9f15-45f4-a886-740b351a39b6. PubMed PMID: 24244340; PubMed Central PMCID: PMC3823839.