产品描述: IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. |
靶点:
IC50: 22 nM (PHD2);HIF/HIFProlyl-Hydroxylase |
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 |
参考文献:
1. Chowdhury R, et al. Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. ACS Chem Biol. 2013 Jul 19;8(7):1488-96. 2. Deppe J, et al. Impairment of hypoxia-induced HIF-1α signaling in keratinocytes and fibroblasts by sulfur mustard is counteracted by a selective PHD-2 inhibitor. Arch Toxicol. 2016 May;90(5):1141-50. |
溶解性:
DMSO : 25 mg/mL (70.95 mM; Need ultrasonic) |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.838 ml |
14.191 ml |
28.382 ml |
5 mM |
0.568 ml |
2.838 ml |
5.676 ml |
10 mM |
0.284 ml |
1.419 ml |
2.838 ml |
50 mM |
0.057 ml |
0.284 ml |
0.568 ml |
|
注意: |
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