BC-LI-0186

SKU: orb1298035

Description

BC-LI-0186 is a potent, selective inhibitor of the LRS-RagD interaction with a Kd of 42.1 nM. It suppresses mTORC1 signaling by this mechanism, inhibiting the growth of rapamycin-resistant cancer cells in vitro, and is applied in lung cancer research.

Key Properties

• CAS Number: 695207-56-8
• MW: 429.53
• Purity: 99.71% (May vary between batches)
• Formula: C₂₂H₂₇N₃O₄S
• SMILES: CC(C)c1c(C)n(C)n(-c2ccc(cc2)S(=O)(=O)NCCOc2ccccc2)c1=O
• Target: Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.31 mM);DMSO:100 mg/mL (232.81 mM)

Bioactivity

• Target IC50:
  LeuRS-RagD:42.1 nM(Kd)|LeuRS-RagD:46.11 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.
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, leucyl-tRNA synthetase, Leucyl-tRNA synthetase, H460, lung cancer, KRAS G12D, inhibit, A549, 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide, BC LI 0186, BC-LI 0186, BCLI0186, BC-LI0186, BC-LI-0186, Aminoacyl-tRNA Synthetase, RagD, rapamycin-resistant, Ras-related GTP-binding protein D (RagD), tRNA Synthetase, aaRS

Compound Identifiers

PubChem CID

4917788