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GSK864,≥98% (HPLC)

别名:(S)-1-(4-氟苄基)-N3-(4-甲氧基-3,5-二甲基苯基)-7-甲基-5-(1H-吡咯-2-羰基)-4,5,6,7- 四氢-1H-吡唑并[4,3-c]吡啶-3,7-二甲酰胺;(S)-1-(4-Fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide

Empirical Formula (Hill Notation): C30H31FN6O4 CAS号: 1816331-66-4 分子量: 558.60 PubChem化学物质编号: 329826055 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML1757
CAS号: 1816331-66-4
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$677.09

说明

包装

5, 25 mg in glass bottle
 

生化/生理作用

GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. It appears that GSK864 binds to an allosteric binding site and locks WT and mutant IDH1s in a catalytically inactive conformation. GSK864 is a highly bioavailable analog of GSK321. For full characterization details, please visit the GSK864 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
GSK864 helps to decrease cell viability and stimulates apoptosis of tumor cells.
 
GSK864 是异柠檬酸脱氢酶 1 (IDH1) 的细胞渗透性、强效和选择性变构抑制剂,可有效抑制 HT-1080 细胞中细胞内 2-羟基戊二酸 (2-HG) 的产生。 GSK864 似乎与变构结合位点结合,并将 WT 和突变体 IDH1 锁定在无催化活性的构象中。 GSK864 是 GSK321 的高生物利用度类似物。
 

特点和优势

GSK864 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.
This compound is a featured product for Nitric Oxide & Cell Stress research. Click here to discover more featured Nitric Oxide & Cell Stress products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
 

其他说明

GSK864 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK864 probe summary on the Chemical Probes Portal website.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

旋光性

[α]/D -66 to -76°, c = 0.5 in methanol

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

储存温度

2-8°C

SMILES string

O=C(C1=CC=CN1)N2C[C@@](C(N)=O)(C)C(N(CC3=CC=C(F)C=C3)N=C4C(NC5=CC(C)=C(OC)C(C)=C5)=O)=C4C2

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 60 | 欧洲Eur. ≥ 21 | 東京Tokyo ≥ 5 | 香港与北京 ≥ 10