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BC-LI-0186

品牌
Sigma-Aldrich
CAS
695207-56-8
货号
SML2226
规格纯度
≥98% (HPLC)
参考价格
1051.31 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

生化/生理作用

BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM) without affecting LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 inhibits Leu-dependent LRS lysosomal membrane localization (10 μM), RagD GTPase and mTORC1 activation (IC50 = 81.4 nM against Leu-induced S6K phosphorylation), but not ARF1 activation, AKT S473 phosphorylation, Glu- or Arg-dependent S6K phosphorylation, nor the cytosolic and mitochondrial LRS catalytic activities. BC-LI-0186 effectively suppresses the growth of rapamycin-resistant MCT116 MM cancer cells with mTOR-S2035I mutation both in cultures (GI50 = 42.03) and in mice in vivo (by 40% in 2 wks; 20 mg/kg/day i.p.).

基本信息

经验(实验)分子式C22H27N3O4S
分子量429.53
NACRESNA.77

产品性质

测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度2-8℃
SMILES stringO=C(C(C(C)C)=C(C)N1C)N1C2=CC=C(S(NCCOC3=CC=CC=C3)(=O)=O)C=C2

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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