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BC-LI-0186

Katalog-Nr.GC50572

BC-LI-0186 ist ein potenter und selektiver Inhibitor der Interaktion von Leucyl-tRNA-Synthetase (LRS; LeuRS) und Ras-verwandtem GTP-bindendem Protein D (RagD) (IC50 = 46,11 nM). BC-LI-0186 bindet kompetitiv an die RagD-Interaktionsstelle von LRS (Kd = 42,1 nM) und hat Auswirkungen auf LRS-Vps34, LRS-EPRS, RagB-RagD-Assoziation, mTORC1-Komplexbildung oder die AktivitÄten von 12 Kinasen. BC-LI-0186 kann die AktivitÄt von krebsassoziierten MTOR-Mutanten und das Wachstum von Rapamycin-resistenten Krebszellen wirksam unterdrÜcken. BC-LI-0186 ist ein vielversprechender Wirkstoff fÜr die Lungenkrebsforschung.

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BC-LI-0186 Chemische Struktur

Cas No.: 695207-56-8

Größe Preis Lagerbestand Menge
5 mg
91,00 $
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25 mg
334,00 $
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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