IOX2  931398-72-0

IOX-2
分子式：C19H16N2O5   分子量：352.34
 
產(chǎn)品描述
IOX2 是有效的HIF-1α prolyl hydroxylase-2 (PHD2)抑制劑，IC50為21 nM,比作用于JMJD2A, JMJD2C, JMJD2E, JMJD3, 和2OG氧合酶FIH選擇性高100倍以上。
靶點(diǎn)
PHD2
         
IC50
21 nM
         
體外研究
IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.Hypoxia Inducible Factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteosome. 1,2 HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.
體內(nèi)研究
 
溶解性
DMSO 7 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO