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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-mTOR-BC-LI-0186
BC-LI-0186

Chemical Structure : BC-LI-0186

CAS No.: 695207-56-8

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BC-LI-0186 (LeuRS inhibitor BC-LI-0186)

货号: PC-38333Not For Human Use, Lab Use Only.

BC-LI-0186 is a potent, specific inhibitor of Leucyl-tRNA synthetase (LRS), inhibits the leucine-dependent mTORC1 pathway.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3680 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BC-LI-0186 is a potent, specific inhibitor of Leucyl-tRNA synthetase (LRS, LeuRS), inhibits the leucine-dependent mTORC1 pathway.
BC-LI-0186 binds to the RagD interacting site of LRS with KD of 42.1 nM, thereby inhibiting lysosomal localization of LRS and mTORC1 activity.
BC-LI-0186 specifically inhibiting the GTPase activating function of LRS, while not affecting the catalytic activity.
BC-LI-0186binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity.
BC-LI-0186 inhibited cancer cell growth human colon cancer SW620 cells with GI50 of 11 nM, inhibited mTORC1 activity, accompanied by PARP or procaspase-3 cleavage.
BC-LI-0186 inhibited the mTORC1 pathway via LRS even in the presence of the known cancer-associated MTOR mutations, overcome acquired rapamycin resistance both in vitro and in vivo.

物理化学性质&存储条件

分子量 429.535
分子式 C22H27N3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 1 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide

参考文献

1. Choi H, et al. Biochem Biophys Res Commun. 2017 Nov 18;493(2):1129-1135.

2. Kim JH, et al. Nat Commun. 2017 Sep 29;8(1):732.

3. Son K, et al. J Clin Invest. 2019 Apr 15;129(5):2088-2093.

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