FM19G11

FM19G11用途

FM19G11 是一种 hypoxia-inducible factor-1-alpha (HIF-1α) 抑制剂,在 HeLa 细胞中抑制缺氧诱导的荧光素酶活性,其 IC50 值为 80 nM。当 HIF-1α 途径在常氧条件下失活时,FM19G11 会调节其他信号途径,包括 mTOR 和 PI3K/Akt/eNOS。

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FM19G11名称

[ CAS 号 ]:
329932-55-0

[ 中文名 ]:
3-[(2,4-二硝基苯甲酰基)氨基]-苯甲酸2-(4-甲基苯基)-2-氧乙基酯

[ 英文名 ]:
FM19G11

[英文别名 ]:

fm19g11

FM19G11生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> HIF/HIF脯氨酰-羟化酶

研究领域 >> 神经疾病

[ 靶点 ]

HIF-1α[1]

[体外研究]

FM19G11(30-300nm)抑制HeLa细胞系中的HIFα蛋白[1]。FM19G11(500 n m)促进缺氧条件下少突胶质细胞分化[1]。FM19G11(300 nM；3天)显著抑制缺氧GBM-XD、缺氧T98G和常氧T98G细胞中O6-甲基鸟嘌呤DNA甲基转移酶(MGMT)的mRNA水平[2]。M19G11(300 nM；3天)显著增强替莫唑胺(TMZ)的促凋亡作用,尽管FM19G11本身并不诱导凋亡[2]。细胞活力测定[2]细胞系：GBM-XD和T98G细胞浓度：300 nM孵育时间：3天结果：低氧培养中两种细胞株MGMT表达均显著抑制。正常氧培养的98G细胞中MGMT表达下调。细胞活力测定[2]细胞系：GBM-XD和T98G细胞浓度：300nm孵育时间：3天结果：自身无细胞毒性。增强TMZ对缺氧GBM-XD细胞、缺氧T98G细胞和常氧T98G细胞的细胞毒性。

[体内研究]

FM19G11(髓内注射；1-8周)改善严重脊髓损伤(SCI)的运动能力[3]。FM19G11(髓内注射；8周)诱导GAP43(轴突生长标记物)和RIP(损伤处有髓少突胶质细胞标记物)的表达[3]。

[参考文献]

[1]. Victoria MM, et, al. FM19G11, a new hypoxia-inducible factor (HIF) modulator, affects stem cell differentiation status. J Biol Chem. 2010 Jan 8; 285(2): 1333-42.

[2]. You CG, et, al. FM19G11 inhibits O 6 -methylguanine DNA-methyltransferase expression under both hypoxic and normoxic conditions. Cancer Med. 2018 May 15; 7(7): 3292-3300.

[3]. Ana AA, et, al. FM19G11 and Ependymal Progenitor/Stem Cell Combinatory Treatment Enhances Neuronal Preservation and Oligodendrogenesis after Severe Spinal Cord Injury. Int J Mol Sci. 2018 Jan 9; 19(1): 200.

FM19G11物理化学性质

[ 分子式 ]:
C₂₃H₁₇N₃O₈

[ 分子量 ]:
463.39600

[ 精确质量 ]:
463.10200

[ PSA ]:
167.60000

[ LogP ]:
5.53380

[ 外观性状 ]:
powder，off-white to light brown

[ 储存条件 ]:
2-8°C

FM19G11MSDS

详细MSDS(安全技术说明书)

FM19G11安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

FM19G11合成路线

详细合成路线

FM19G11上下游产品

FM19G11上游产品

FM19G11下游产品

FM19G11文献

A novel effect of DMOG on cell metabolism: direct inhibition of mitochondrial function precedes HIF target gene expression.

Biochim. Biophys. Acta 1847 , 1254-66, (2015)

Abnormal accumulation of oncometabolite fumarate and succinate is associated with inhibition of mitochondrial function and carcinogenesis. By competing with α-ketoglutarate, oncometabolites also activ...

Loss of SIRT3 Provides Growth Advantage for B Cell Malignancies.

J. Biol. Chem. 291 , 3268-79, (2016)

B cell malignancies comprise a diverse group of cancers that proliferate in lymph nodes, bone marrow, and peripheral blood. SIRT3 (sirtuin 3) is the major deacetylase within the mitochondrial matrix t...

Downregulation of duodenal SLC transporters and activation of proinflammatory signaling constitute the early response to high altitude in humans.

Am. J. Physiol. Gastrointest. Liver Physiol. 307(7) , G673-88, (2014)

Solute carrier (SLC) transporters mediate the uptake of biologically active compounds in the intestine. Reduced oxygenation (hypoxia) is an important factor influencing intestinal homeostasis. The aim...

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