Home Cell Cycle DNA/RNA Synthesis inhibitor BC-LI-0186 For research use only.

BC-LI-0186

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.

BC-LI-0186 Chemical Structure

BC-LI-0186 Chemical Structure

CAS: 695207-56-8

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

Purity & Quality Control

Batch: E048801 DMSO] 86 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.30%
99.30

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models K-ras mouse lung cancer model, LSL K-ras G12D lung cancer mouse model
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 429.53 Formula

C22H27N3O4S
CAS No. 695207-56-8 SDF --
Smiles CC(C)C1=C(C)N(C)N(C1=O)C2=CC=C(C=C2)[S](=O)(=O)NCCOC3=CC=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (200.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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