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Description: Leucyl-tRNA synthase (TRS)/Ras-related GTP-binding protein D (RagD) interaction inhibitor
Chemical Name: 4-[2,5-Dihydro-2,3-dimethyl-4-(1-methylethyl)-5-oxo-1H-pyrazol-1-yl]-N-(2-phenoxyethyl)benzenesulfonamide
Purity: ≥98% (HPLC)

Biological Activity for BC-LI-0186

BC-LI-0186 is a 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.

Compound Libraries for BC-LI-0186

BC-LI-0186 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for BC-LI-0186

M. Wt 429.54
Formula C22H27N3O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 695207-56-8
PubChem ID 4917788
Smiles CC(C1=C(N(N(C2=CC=C(S(=O)(NCCOC3=CC=CC=C3)=O)C=C2)C1=O)C)C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BC-LI-0186

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 42.95 100

Preparing Stock Solutions for BC-LI-0186

The following data is based on the product molecular weight 429.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.64 mL 23.28 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
10 mM 0.23 mL 1.16 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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References for BC-LI-0186

References are publications that support the biological activity of the product.

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

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Keywords: BC-LI-0186, BC-LI-0186 supplier, Leucyl-RNA, synthase, TRS, RagD, GTPase, interaction, inhibitor, mTOR, complex, translocation, lysosome, Other, Synthases/Synthetases, Ras, GTPases, 6791, Tocris Bioscience

Citations for BC-LI-0186

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