bs-60284C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 328.33

Formula: C15 H16 N6 O3

CAS Number: 1154097-71-8

InChi Key: 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

Smiles: CC(C)(C)OC(=O)C1=CN=C(C=C1)N1NC=C(C1=O)N1C=CN=N1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

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.