931398-72-0
931398-72-0 結(jié)構(gòu)式
基本信息
脯氨酰羥化酶-2抑制劑(PHD2抑制劑)(IOX2)
2-(1-芐基-4-羥基-2-氧代-1,2-二氫喹啉-3-甲酰氨基)乙酸
N-[[4-羥基-2-氧代-1-(苯基甲基)-1,2-二氫-3-喹啉基]羰基]甘氨酸
N-[[4-羥基-2-氧代-1-(苯基甲基)-1,2-二氫-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
物理化學性質(zhì)
常見問題列表
| Target | Value |
|
PHD2
(Cell-free assay) | 21 nM |
IOX2有效抑制PHD2 (IC50為21 nM)，比抑制JMJD2A, JMJD2C, JMJD2E, JMJD3, 或2OG加氧酶FIH(IC50<100 μM)選擇性高100多倍。IOX2有效作用于細胞，50 μM時，作用于RCC4細胞，抑制HIF-1α羥化。 缺氧誘導因子（HIF）通過在HIF-1α亞單位，由脯氨酰殘基在氧依賴性降解結(jié)構(gòu)域的羥化調(diào)節(jié)。1,2 HIF 脯氨酰羥基化是由脯氨酰羥化酶結(jié)構(gòu)域酶(PHD1, 2, 和 3), Fe(II) 和 2-酮戊二酸 (2OG) 加氧酶家族成員催化。他們需要分子氧作為輔助底物，從而充當HIF系統(tǒng)的缺氧敏感元件。缺氧抑制PHD活性，增加HIF轉(zhuǎn)錄復合物的豐度和活性。
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.