推荐产品
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(C(C(C)C)=C(C)N1C)N1C2=CC=C(S(NCCOC3=CC=CC=C3)(=O)=O)C=C2
InChI
1S/C22H27N3O4S/c1-16(2)21-17(3)24(4)25(22(21)26)18-10-12-20(13-11-18)30(27,28)23-14-15-29-19-8-6-5-7-9-19/h5-13,16,23H,14-15H2,1-4H3
InChI key
SQYWMHPZMHDCHP-UHFFFAOYSA-N
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.).
Leucyl-tRNA synthetase (LRS) and RagD interaction blocker that inhibits Leu-dependent LRS lysosomal localization, RagD and mTOR activation.
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
Hyosun Choi et al.
Biochemical and biophysical research communications, 493(2), 1129-1135 (2017-09-09)
Leucyl-tRNA synthetase (LRS) plays major roles in providing leucine-tRNA and activating mechanistic target of rapamycin complex 1 (mTORC1) through intracellular leucine sensing. mTORC1 activated by amino acids affects the influence on physiology functions including cell proliferation, protein synthesis and autophagy
Jong Hyun Kim et al.
Nature communications, 8(1), 732-732 (2017-10-01)
Leucyl-tRNA synthetase (LRS) is known to function as leucine sensor in the mammalian target of rapamycin complex 1 (mTORC1) pathway. However, the pathophysiological significance of its activity is not well understood. Here, we demonstrate that the leucine sensor function for mTORC1
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.
联系技术服务部门