Product Name :
IOX4, PHD2 Inhibitor
Description:
IOX4 is a potent and selective PHD2 inhibitor with IC50 ~1.6 nM. It inhibits PHD2 via binding to the 2OG binding site, 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 ~5.6-11.7 µM) and inducing HIF-1α and HIF-2α 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. IOX4 could be a useful tool compound for studies aimed at validating the upregulation of HIF for treatment of cerebral diseases including stroke.
CAS:
1154097-71-8
Molecular Weight:
328.33
Formula:
C15H16N6O3
Chemical Name:
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
Smiles :
CC(C)(C)OC(=O)C1=CN=C(C=C1)N1NC=C(C1=O)N1C=CN=N1
InChiKey:
HWQQDVNGHZIALS-UHFFFAOYSA-N
InChi :
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IOX4 is a potent and selective PHD2 inhibitor with IC50 ~1.6 nM. It inhibits PHD2 via binding to the 2OG binding site, displays >1, 000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO.{{Lincomycin hydrochloride} MedChemExpress|{Lincomycin hydrochloride} Anti-infection|{Lincomycin hydrochloride} Biological Activity|{Lincomycin hydrochloride} Purity|{Lincomycin hydrochloride} custom synthesis|{Lincomycin hydrochloride} Cancer} IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 ~5.{{Podofilox} MedChemExpress|{Podofilox} Cytoskeleton|{Podofilox} Purity & Documentation|{Podofilox} Purity|{Podofilox} supplier|{Podofilox} Autophagy} 6-11.7 µM) and inducing HIF-1α and HIF-2α 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. IOX4 could be a useful tool compound for studies aimed at validating the upregulation of HIF for treatment of cerebral diseases including stroke.PMID:23667820 |Product information|CAS Number: 1154097-71-8|Molecular Weight: 328.33|Formula: C15H16N6O3|Chemical Name: tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate|Smiles: CC(C)(C)OC(=O)C1=CN=C(C=C1)N1NC=C(C1=O)N1C=CN=N1|InChiKey: HWQQDVNGHZIALS-UHFFFAOYSA-N|InChi: 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|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|IOX4 was used at 10-50 µM final concentration in vitro and in cellular assays.|In Vivo:|IOX4 was dosed to mice by IP injection at 17.5-70 mg/kg.|References:|Chan MC, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. (2015) PLoS One. 10(7):e0132004.Products are for research use only. Not for human use.|Documents||