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.
CAS Number: 931398-72-0
Molecular Weight: 352.34
Chemical Name: 2-(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid
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
IOX2 was usually used at 10-50µM final concentration in vitro.
- 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.
- 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.
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