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BC-LI-0186

Catalog No. T9533 CAS 695207-56-8

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

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) 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.

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BC-LI-0186, CAS 695207-56-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 272.00
50 mg	In stock	$ 428.00
100 mg	In stock	$ 639.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.17%

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Description	BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) 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.
Targets&IC50	LeuRS-RagD:42.1 nM(Kd), LeuRS-RagD:46.11 nM
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)[1]. 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[1]. 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[1].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)[1].
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[1].

Synonyms	4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
Molecular Weight	429.53
Formula	C22H27N3O4S
CAS No.	695207-56-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (232.81 mM)

References and Literature

1. Jong Hyun Kim, et al. Control of leucine-dependent mTORC1 pathway through chemical intervention of leucyl-tRNA synthetase and RagD interaction. Nat Commun. 2017 Sep 29;8(1):732. 2. Choi H, Son JB, Kang J, Kwon J, Kim JH, Jung M, Kim SK, Kim S, Mun JY. Leucine-induced localization of Leucyl-tRNA synthetase in lysosome membrane. Biochem Biophys Res Commun. 2017 Nov 18;493(2):1129-1135. 3. Lee M, Kim JH, Yoon I, Lee C, Fallahi Sichani M, Kang JS, Kang J, Guo M, Lee KY, Han G, Kim S, Han JM. Coordination of the leucine-sensing Rag GTPase cycle by leucyl-tRNA synthetase in the mTORC1 signaling pathway. Proc Natl Acad Sci U S A. 2018 Jun 5;115(23):E5279-E5288.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library PPI Inhibitor Library Anti-Lung Cancer Compound Library Anti-Cancer Compound Library

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Keywords

BC-LI-0186 695207-56-8 Others Aminoacyl-tRNA Synthetase RagD BC-LI0186 rapamycin-resistant BCLI0186 tRNA Synthetase, aaRS H460 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide KRAS G12D A549 lung cancer BC LI 0186 inhibit BC-LI 0186 Inhibitor Leucyl-tRNA synthetase inhibitor

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