BC-LI-0186 |
| Catalog No.GC50572 |
BC-LI-0186 est un inhibiteur puissant et sélectif de l'interaction entre la leucyl-ARNt synthétase (LRS; LeuRS) et la protéine D de liaison au GTP (RagD) liée À Ras (IC50 = 46,11 nM). BC-LI-0186 se lie de manière compétitive au site d'interaction RagD du LRS (Kd = 42,1 nM) et a des effets sur LRS-Vps34, LRS-EPRS, l'association RagB-RagD, la formation du complexe mTORC1 ou les activités de 12 kinases. BC-LI-0186 peut supprimer efficacement l'activité des mutants MTOR associés au cancer et la croissance des cellules cancéreuses résistantes À la rapamycine. BC-LI-0186 est un agent prometteur pour la recherche sur le cancer du poumon.
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.
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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
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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