IOX4

IOX4 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2, IC50 = 1.6 nM). 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-1alpha levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1alpha and HIF-2alpha expression in mice. 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.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: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 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.