IOX2, HIF Prolyl-Hydroxylases (PHD2) Inhibitor

IOX2 is a potent, selective and cell permeable inhibitor of hypoxia inducible factor 1α (HIF1α) prolyl hydroxylase-2 (PHD2). It inhibits PHD2 with an IC50 ~21 nM, and exhibits over 100-fold selectivity against JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.

Product information

CAS Number: 931398-72-0

Molecular Weight: 352.34

Formula: C19H16N2O5

Chemical Name: 2-(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid

Smiles: OC(=O)CNC(=O)C1C(=O)N(CC2C=CC=CC=2)C2=CC=CC=C2C=1O

InChiKey: CAOSCCRYLYQBES-UHFFFAOYSA-N

InChi: InChI=1S/C19H16N2O5/c22-15(23)10-20-18(25)16-17(24)13-8-4-5-9-14(13)21(19(16)26)11-12-6-2-1-3-7-12/h1-9,24H,10-11H2,(H,20,25)(H,22,23)

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: ≥360 days 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:

IOX2 was usually used at 10-50µM final concentration in vitro.

References:

1. Murray JK, et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. (2010) J Comb Chem. 12(5):676-86.
2. SGC website: http://www.thesgc.org/scientists/chemical_probes/IOX2
3. Tian YM, et al. Differential sensitivity of hypoxia inducible factor hydroxylation sites to hypoxia and hydroxylase inhibitors. (2011) J Biol Chem. 286(15):13041-51.

Products are for research use only. Not for human use.