931398-72-0
931398-72-0 结构式
基本信息
脯氨酰羟化酶-2抑制剂(PHD2抑制剂)(IOX2)
2-(1-苄基-4-羟基-2-氧代-1,2-二氢喹啉-3-甲酰氨基)乙酸
N-[[4-羟基-2-氧代-1-(苯基甲基)-1,2-二氢-3-喹啉基]羰基]甘氨酸
N-[[4-羟基-2-氧代-1-(苯基甲基)-1,2-二氢-3-喹啉基]羰基]甘氨酸(IOX-2)
JICL38
CS-564
IOX 2, >=98%
IOX2(Glycine)
IOX-2
IOX2
IOX 2
IOX2
IOX 2
IOX-2
JICL38
(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)glycine
2-[(1-BENZYL-4-HYDROXY-2-OXOQUINOLINE-3-CARBONYL)AMINO]ACETIC ACID
2-(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxaMido)acetic acid
物理化学性质
常见问题列表
| Target | Value |
|
PHD2
(Cell-free assay) | 21 nM |
IOX2有效抑制PHD2 (IC50为21 nM)，比抑制JMJD2A, JMJD2C, JMJD2E, JMJD3, 或2OG加氧酶FIH(IC50<100 μM)选择性高100多倍。IOX2有效作用于细胞，50 μM时，作用于RCC4细胞，抑制HIF-1α羟化。 缺氧诱导因子（HIF）通过在HIF-1α亚单位，由脯氨酰残基在氧依赖性降解结构域的羟化调节。1,2 HIF 脯氨酰羟基化是由脯氨酰羟化酶结构域酶(PHD1, 2, 和 3), Fe(II) 和 2-酮戊二酸 (2OG) 加氧酶家族成员催化。他们需要分子氧作为辅助底物，从而充当HIF系统的缺氧敏感元件。缺氧抑制PHD活性，增加HIF转录复合物的丰度和活性。
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.