Cas No.: | 1154097-71-8 |
Chemical Name: | Tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate |
Synonyms: | IOX4 NEW;IOX4;tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate;BDBM118338;ZB1530;US8653111, 62;tert-butyl 6-[3-oxo-4-(triazol-1-yl)-1H-pyrazol-2-yl]pyridine-3-carboxylate |
SMILES: | O(C(C1=C([H])N=C(C([H])=C1[H])N1C(C(=C([H])N1[H])N1C([H])=C([H])N=N1)=O)=O)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] |
Formula: | C15H16N6O3 |
M.Wt: | 328.3259 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2[1]. |
In Vitro: | IOX4 (1-100 μM; 5 hours) determines the EC50s for HIF1α induction are 114 μM, 86 μM and 49.5 μM in MCF-7, Hep3B and U2OS, respectively[1]. |
References: | [1]. Chan MC, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004. |