产品信息
抗原名称
HIF_HIF Prolyl-Hydroxylase
商品描述
IOX 2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) (IC50 = 21 nM). IOX 2 displays over 100-fold selectivity for PHD2 over factor inhibiting HIF-1 (FIH-1) and histone demethylases.
分子量
352.34
纯度
>98%
可溶性
DMSO ：7 mg/mL (19.86 mM)
外观
white to beige powder
In vitro(体外研究)
IOX2 is at least 2-5000 fold selective, as judged by IC50 values, for PHD2 over the KDMs and Factor Inhibiting HIF(FIH). IOX2 significantly upregulates the transcription of VEGF-A and BNIP3 in normal human epidermal keratinocytes (NHEK) and normal human dermal fibroblasts (NHDF) when grown under normoxia and hypoxia. IOX2 efficiently promotes HIF-1α stability, nuclear translocation, and target gene expression in keratinocytes and fibroblasts. In addition, IOX2 significantly upregulates biosynthesis and transcription of VEGF-A and BNIP3 in sulfur mustard (SM)-exposed NHEK and NHDF grown under hypoxia. These results suggest that application of IOX2 is useful for restoring of SM-affected HIF-1α stability and signaling activity in keratinocytes and fibroblasts.
In vivo(体内研究)
To investigate the utility of IOX2 as in vivo functional probes, IOX2 is tested to upregulate HIF signaling in a whole organism, that is, transgenic zebrafish (Danio rerio). Because the expression of the PHD3 encoding gene is regulated by HIF in humans and zebrafish, PHD3 levels are a readout of HIF activity. A zebrafish hypoxia reporter line is generated expressing GFP with the phd3 promoter elements. Transgenic wild-type embryos at 3 days postfertilization treated with compounds (10 μM) for 2 days displayed clear increase in phd3:EGFP expression in the liver, relative to controls. Significant increases in GFP levels are observed with IOX2.
背景
分子式
C19H16N2O5
CAS号
931398-72-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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