2. Metabolic Enzyme/Protease
  3. Aminoacyl-tRNA Synthetase
  4. BC-LI-0186

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.

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BC-LI-0186 Chemical Structure

BC-LI-0186 Chemical Structure

CAS No. : 695207-56-8

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Based on 1 publication(s) in Google Scholar

BC-LI-0186 Related Antibodies

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Description

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research[1][2].

IC50 & Target

IC50: 46.11 nM (LeuRS and RagD interaction)[1]
Kd: 42.1 nM (LeuRS and RagD interaction)[1]
In Vitro

BC-LI-0186 (0-20 μM; starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min) inhibits phosphorylation of S6K in a dose- and time-dependent manner, but it has no effects on hosphorylation of AKT (S473)[1].
BC-LI-0186 (0-20 μM; 6 hours) induces cleaved poly (ADP-ribose) polymerase (PARP) and caspase-3 and an increase of p62 in A549 and H460 cells[1].
BC-LI-0186 exhibits cytotoxic effect at nanomolar concentration in NSCLC cells, 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 overcome 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BC-LI-0186 Related Antibodies

Cell Viability Assay[1]

Cell Line: NSCLC cells
Concentration: 0 μM, 0.1 μM, 0.2 μM,1 μM, 2 μM, 5 μM, 10 μM, 20 μM
Incubation Time: Starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min
Result: Suppressed leucine-mediated mTORC1 activation in NSCLC cells.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: K-ras mouse lung cancer modelan LSL K-ras G12D lung cancer animal model[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week
Result: Showed activated caspase-3-positive cells higher in the BC-LI-0186-treated group than in the vehicle or cisplatin-treated group.
Reduced p-S6 and p-AKT level whereas cisplatin alone has minimal effect on both p-S6 and p-AKT expression.
Showed a slight (not statistically significant) increase in body weight during the treatment period.
Exhibited a specific inhibition of mTORC1 and not mTORC2.
Molecular Weight

429.53

Formula

C22H27N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N2N(C)C(C)=C(C(C)C)C2=O)C=C1)(NCCOC3=CC=CC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (291.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3281 mL 11.6406 mL 23.2813 mL
5 mM 0.4656 mL 2.3281 mL 4.6563 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3281 mL 11.6406 mL 23.2813 mL 58.2032 mL
5 mM 0.4656 mL 2.3281 mL 4.6563 mL 11.6406 mL
10 mM 0.2328 mL 1.1641 mL 2.3281 mL 5.8203 mL
15 mM 0.1552 mL 0.7760 mL 1.5521 mL 3.8802 mL
20 mM 0.1164 mL 0.5820 mL 1.1641 mL 2.9102 mL
25 mM 0.0931 mL 0.4656 mL 0.9313 mL 2.3281 mL
30 mM 0.0776 mL 0.3880 mL 0.7760 mL 1.9401 mL
40 mM 0.0582 mL 0.2910 mL 0.5820 mL 1.4551 mL
50 mM 0.0466 mL 0.2328 mL 0.4656 mL 1.1641 mL
60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9701 mL
80 mM 0.0291 mL 0.1455 mL 0.2910 mL 0.7275 mL
100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5820 mL
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BC-LI-0186 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BC-LI-0186695207-56-8Aminoacyl-tRNA SynthetasetRNA Synthetase, aaRSLeucyl-tRNA synthetaseRagDrapamycin-resistantlung cancerA549H460KRAS G12DInhibitorinhibitorinhibit

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