BC-LI-0186
CAS No. 695207-56-8
BC-LI-0186 ( 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide )
产品货号. M28745 CAS No. 695207-56-8
BC-LI-0186 is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM.
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥356 | 有现货 |
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5MG | ¥583 | 有现货 |
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10MG | ¥988 | 有现货 |
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25MG | ¥2203 | 有现货 |
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50MG | ¥3467 | 有现货 |
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100MG | ¥5176 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称BC-LI-0186
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述BC-LI-0186 is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM.
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产品描述BC-LI-0186 is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.(In Vitro):Administration of 0-20 μM BC-LI-0186 followed by starved for 90?min in the leucine-free medium and then in the serum-free media for 15?min inhibits phosphorylation of S6K dose- and time-dependently, but it has no effects on phosphorylation of AKT (S473). Administration of 0-20 μM BC-LI-0186 for 6 hours induces cleaved poly ADP-ribose polymerase (PARP) and caspase-3 and an increase of p62 in A549 and H460 cells. In NSCLC cells, BC-LI-0186 exhibits cytotoxic effect at nanomolar concentration, it exhibits IC50 values of 98 nM, 206 nM, 55 nM, 78 nM, 83 nM, 86 nM, 102 nM, 109 nM, 128 nM, and 206 nM in A549, H460, H2228, H1703, SNU1330, H1650, H2009, H358, H2279, H460, and H596 cells, respectively.BC-LI-0186 overcomes acquired rapamycin resistance and inhibits the mTORC1 pathway in isogenic HCT116 cell lines that harbored either M TOR WT (HCT116 MW) or S2035I mutations (HCT116 MM), it exhibits little changed efficacy between the wild-type and mutant cells (GI50:39.49 ?nM and 42.03?nM, EC50:105.03 nM and 100.45 ?nM).(In Vivo):Intraperitoneal injection of 50?mg/kg BC-LI-0186 alone or combines with cisplatin alone for 2 weeks(bid for 5?days per week) exhibits antitumor effects and significantly reduces tumor size compared with treatment with vehicle in an LSL K-ras G12D lung cancer animal model.
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同义词4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
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通路Others
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靶点Other Targets
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受体H1 receptor
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研究领域——
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适应症——
化学信息
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CAS Number695207-56-8
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分子量858.1
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分子式C44H53N6O8S2
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纯度>98% (HPLC)
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溶解度——
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SMILESCC(C)C(C1=O)=C(C)N(C)N1c(cc1)ccc1S(NCCOc1ccccc1)(=O)=OCC(C)C(C1=O)=C(C)N(C)N1c(cc1)ccc1S(NCCOc1ccccc1)(=O)=O
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Abou-Gharbia M, et al. New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. J Med Chem. 1995 Sep 29;38(20):4026-32.
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