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BC-LI-0186

Chemical Structure : BC-LI-0186

CAS No.: 695207-56-8

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

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 429.535
Formula C22H27N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 1 Months
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

References

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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