BC-LI-0186 是一种有效的选择性亮氨酰-tRNA 合成酶 (LRS; LeuRS) 和 Ras 相关的 GTP 结合蛋白 D (RagD) 相互作用的抑制剂 (IC50=46.11 nM)。 BC-LI-0186 竞争性结合 LRS 的 RagD 相互作用位点 (Kd=42.1 nM)，并影响 LRS-Vps34、LRS-EPRS、RagB-RagD 结合、mTORC1 复合物形成或 12 种激酶的活性。 BC-LI-0186 可以有效抑制癌症相关的 MTOR 突变体的活性和雷帕霉素耐药癌细胞的生长。 BC-LI-0186 是一种很有前途的肺癌研究药物。
| Cas No. | 695207-56-8 |
| 别名 | 4-(4-异丙基-2,3-二甲基-5-氧代-2,5-二氢-1H-吡唑-1-基)-N-(2-苯氧基乙基)苯磺酰胺 |
| Canonical SMILES | CC(C1=C(N(N(C2=CC=C(S(=O)(NCCOC3=CC=CC=C3)=O)C=C2)C1=O)C)C)C |
| 分子式 | C22H27N3O4S |
| 分子量 | 429.54 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 |
