跳转至内容
Merck
CN

SML0895

Sigma-Aldrich

AGI-6780

≥98% (HPLC)

别名:

N-Cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide

登录查看公司和协议定价

选择尺寸

关于此项目

经验公式（希尔记法）:
C21H18F3N3O3S2
化学文摘社编号:
1432660-47-3
分子量:
481.51
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

查看所有文档
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to light brown

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

FC(F)(F)c1cc(ccc1)NC(=O)Nc2c(ccc(c2)[S](=O)(=O)NC4CC4)c3c[s]cc3

InChI

1S/C21H18F3N3O3S2/c22-21(23,24)14-2-1-3-16(10-14)25-20(28)26-19-11-17(32(29,30)27-15-4-5-15)6-7-18(19)13-8-9-31-12-13/h1-3,6-12,15,27H,4-5H2,(H2,25,26,28)

InChI key

CCAWRGNYALGPQH-UHFFFAOYSA-N

相关类别

生化/生理作用

AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2.
AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.

特点和优势

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000425773
0000425773
0000380564
0000380564
0000183846

没有发现合适的版本？

如果您需要特殊版本，可通过批号或批次号查找具体证书。

搜索COA

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

Jan Mauer et al.
Nature chemical biology, 15(4), 340-347 (2019-02-20)
Small nuclear RNAs (snRNAs) are core spliceosome components and mediate pre-mRNA splicing. Here we show that snRNAs contain a regulated and reversible nucleotide modification causing them to exist as two different methyl isoforms, m1 and m2, reflecting the methylation state
Kancharana Bala Bhaskara Rao et al.
FEBS letters, 593(16), 2177-2193 (2019-06-19)
Isocitrate dehydrogenases (IDHs) are metabolic enzymes that are mutated in several cancers, resulting in overproduction of d-2-hydroxyglutarate (D-2HG). However, the signalling pathways and factors that regulate mutant IDHs or their metabolites remain elusive. Here, we report that in synchronized cells

商品

Discover Bioactive Small Molecules for Gene Regulation

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系客户支持