A selective, bioavailable inhibitor of HIF-PH2
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IOX4

Item No. 18181

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,1-dimethylethyl ester 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-3-pyridinecarboxylic acid
CAS Number
1154097-71-8
Molecular Formula
C15H16N6O3
Formula Weight
328.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
256, 291 nm
SMILES
CC(C)(C)OC(C1=CN=C(N2NC=C(N3C=CN=N3)C2=O)C=C1)=O
InChi Code
InChI=1S/C15H16N6O3/c1-15(2,3)24-14(23)10-4-5-12(16-8-10)21-13(22)11(9-18-21)20-7-6-17-19-20/h4-9,18H,1-3H3
InChi Key
HWQQDVNGHZIALS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $81

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    10 mg

    $152

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    25 mg

    $357

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    50 mg

    $633

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    Product Description

    IOX4 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 1.6 nM).1 It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.1 The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chan, M.C., Atasoylu, O., Hodson, E., et al. Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain. PLoS One 10(7), e0132004 (2015).