BC-LI-0186

Catalog No.E0488 Batch:E048801

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Technical Data

Formula

C22H27N3O4S
Molecular Weight 429.53 CAS No. 695207-56-8
Solubility (25°C)* In vitro DMSO 86 mg/mL (200.21 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS, LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (LRS-RagD interaction) (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM), thereby inhibiting lysosomal localization of LRS and mTORC1 activity. It also effectively suppresses the activity of cancer-associated mTOR mutants and the growth of rapamycin-resistant cancer cells.
Targets
Leucyl-tRNA synthetase [1]
(in surface plasmon resonance (SPR) analysis)		 Leucyl-tRNA synthetase [1]
(in chemical inhibition assay of the LRS–RagD interaction)
42.1 nM(Kd) 46.11 nM
In vitro

BC-LI-0186 binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity. BC-LI-0186 also effectively suppresses the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells.[1]
In vivo

BC-LI-0186 (intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 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]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Human colon cancer cells, Human pancreatic cancer cells, Human breast cancer cells, Human ovary cancer cells, Human glioblastoma cells

  • Concentrations

    0-20 μM

  • Incubation Time

    15 min

  • Method

    Cells are starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min, or 1.5 h, or 6 h. And the cell lysates are analyzed with the corresponding antibodies.
Animal Study:

[1]
  • Animal Models

    K-ras mouse lung cancer model, LSL K-ras G12D lung cancer mouse model

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Selleck's BC-LI-0186 has been cited by 1 publication

Combination of the LARS1 Inhibitor, BC-LI-0186 with a MEK1/2 Inhibitor Enhances the Anti-Tumor Effect in Non-Small Cell Lung Cancer [ Cancer Res Treat, 2023, 55(3):851-864] PubMed: 36960627

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.