BC-LI-0186 |
カタログ番号GC50572 |
BC-LI-0186 は、ロイシル tRNA 合成酵素 (LRS; LeuRS) および Ras 関連 GTP 結合タンパク質 D (RagD) 相互作用の強力かつ選択的な阻害剤です (IC50=46.11 nM)。 BC-LI-0186 は、LRS の RagD 相互作用部位に競合的に結合し (Kd = 42.1 nM)、LRS-Vps34、LRS-EPRS、RagB-RagD 会合、mTORC1 複合体形成、または 12 種類のキナーゼの活性に影響を与えます。 BC-LI-0186 は、がん関連の MTOR 変異体の活動とラパマイシン耐性がん細胞の増殖を効果的に抑制することができます。 BC-LI-0186 は、肺がん研究の有望な薬剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 695207-56-8
Sample solution is provided at 25 µL, 10mM.
Potent and high affinity leucyl-tRNA synthase (TRS)/Ras-related GTP-binding protein D (RagD) interaction inhibitor (IC50 = 46.1 nM; Kd = 42.1 nM for binding to LRS). Inhibits mTOR complex 1 activity by blocking binding to LRS without affecting catalytic activity. Inhibits leucine-induced translocation of LRS to the lysosome.
Kim et al (2017) Control of leucine-dependent mTORC1 pathway through chemical intervention of leucyl-tRNA synthetase and RagD interaction. Nat.Commun. 8 732 PMID:28963468 |Choi et al (2017) Leucine-induced localization of Leucyl-tRNA synthetase in lysosome membrane. Biochem.Biophys.Res.Commun. 493 1129 PMID:28882589 |Lee et al (2018) Coordination of the leucine-sensing Rag GTPase cycle by leucyl-tRNA synthetase in the mTORC1 signaling pathway. Proc.Natl.Acad.Sci.USA. 115 E5279 PMID:29784813
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