BC-LI-0186 |
| Catalog No.GC50572 |
BC-LI-0186은 Leucyl-tRNA 합성효소(LRS; LeuRS) 및 Ras 관련 GTP-결합 단백질 D(RagD) 상호작용(IC50=46.11nM)의 강력하고 선택적인 억제제입니다. BC-LI-0186은 LRS의 RagD 상호작용 부위(Kd=42.1nM)에 경쟁적으로 결합하고 LRS-Vps34, LRS-EPRS, RagB-RagD 결합, mTORC1 복합체 형성 또는 12개 키나제의 활성에 영향을 미칩니다. BC-LI-0186은 암 관련 MTOR 돌연변이의 활성과 라파마이신 내성 암세포의 성장을 효과적으로 억제할 수 있습니다. BC-LI-0186은 폐암 연구를 위한 유망한 약제입니다.
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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