2. MAPK/ERK Pathway Immunology/Inflammation Autophagy Epigenetics Neuronal Signaling NF-κB Protein Tyrosine Kinase/RTK Stem Cell/Wnt PI3K/Akt/mTOR Metabolic Enzyme/Protease Apoptosis JAK/STAT Signaling
  3. JAK Akt Autophagy p38 MAPK Reactive Oxygen Species (ROS) VEGFR STAT Amyloid-β HIF/HIF Prolyl-Hydroxylase Apoptosis JNK PI3K
  4. Liensinine

Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.

For research use only. We do not sell to patients.

CAS No. : 2586-96-1

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Based on 20 publication(s) in Google Scholar

Other Forms of Liensinine:

Liensinine Related Antibodies

Top Publications Citing Use of Products

    Liensinine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793.  [Abstract]

    The viability of HBE cells treated with different concentration of Liensinine (LIE) (10, 20, 40, 60, 80 μM) measured by CCK8 assay.

    Liensinine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793.  [Abstract]

    Liensinine (LIE) (40 μM) treatment effectively suppressed autophagy by Western blot.

    Liensinine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793.  [Abstract]

    Liensinine (LIE) (40 μM) improved mitochondrial damage induced by ARSK knockdown, as evidenced by the reductions in intracellular and mitochondrial ROS levels.

    Liensinine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793.  [Abstract]

    SA-β-gal staining results demonstrated that Liensinine (LIE) (40 μM) treatment obviously decreased the percentage of positive cells.

    Liensinine purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793.  [Abstract]

    The expressions of IL-6, IL-8 and IL-1β were both relived in HBE cells by Liensinine (LIE) (40 μM).

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    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke[1][2][3][4][5].

    Cellular Effect
    Cell Line Type Value Description References
    3T3-L1 IC50
    19.4 μM
    Compound: 9
    Anti-adipogenic activity in mouse 3T3-L1 cells transfected with Lenti-PPARgamma-Luc reporter assessed as inhibition of PPARgamma expression by luminescence based microplate reader analysis
    Anti-adipogenic activity in mouse 3T3-L1 cells transfected with Lenti-PPARgamma-Luc reporter assessed as inhibition of PPARgamma expression by luminescence based microplate reader analysis
    		[PMID: 38483204]
    In Vitro

    Liensinine (5-80 μM; 24 h) reduces the viability of SaOS-2, MG-63, 143B and U-2OS osteosarcoma cells in a dose-dependent manner, but has no effect on the viability of hFOB 1.19 normal osteoblasts[1].
    Liensinine (40-80 μM; 24 h) inhibits the proliferation and colony-forming ability of SaOS-2 and 143B osteosarcoma cells, induces apoptosis, and causes G0/G1 cell cycle arrest in a dose-dependent manner[1].
    Liensinine (40-80 μM; 24 h) increases intracellular ROS production in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner, but does not affect ROS levels in hFOB 1.19 normal osteoblasts[1].
    Liensinine (40-80 μM; 24 h) disrupts the GSH/GSSG redox balance in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner by decreasing GSH levels, increasing GSSG levels, and elevating the GSSG/GSH ratio[1].
    Liensinine (40-80 μM; 24 h) induces the loss of mitochondrial membrane potential in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner[1].
    Liensinine (40-80 μM; 24 h) dose-dependently regulates the expression of apoptosis- and cell cycle-related proteins in SaOS-2 and 143B osteosarcoma cells in vitro, and inhibits the activation of the JAK2/STAT3 pathway, but exerts no effect on the aforementioned proteins in hFOB 1.19 normal osteoblasts[1].
    Liensinine (20 μM; 24 h) enhances cell viability, reduces apoptosis and cytotoxicity, and inhibits autophagy in an in vitro oxygen-glucose deprivation/reoxygenation ischemia-reperfusion model[3].

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

    Liensinine Related Antibodies
    In Vivo

    Liensinine (20 mg/kg; i.p.; once daily; for 21 consecutive days) significantly inhibits the growth of subcutaneous hepatocellular carcinoma (HCC) xenografts in male BALB/c nude mice, reduces tumor vascular density, and reshapes the tumor immune microenvironment into an anti-tumor phenotype[5].
    Liensinine (20 mg/kg; i.p.; once daily for 16 consecutive days) significantly inhibits orthotopic HCC tumor progression in male C57BL/6 mice, induces tumor metabolic reprogramming, reduces tumor vascular density, regulates macrophage polarization, and downregulates PD-L1 expression[5].

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

    Animal Model: KM mice[2]
    Dosage: 100 mg/kg, 200 mg/kg
    Administration: oral gavage, daily, 10 weeks
    Result: Reduced the gingival index and increased the SOD levels, the CAT, GSH-Px levels and decreased the NO, MDA, and ET levels compared to the control group.
    Animal Model: Institute of Cancer Research (ICR) mice (male, 20-22 g)[3]
    Dosage:
    Administration: 5 mg/kg by oral administration; 1 mg/kg by intravenous administration
    Result: The pharmacokinetic parameters of Liensinine in mice
    Parameters po (5 mg/kg) iv (1 mg/kg)
    AUC(0-t) (ng/mL*h) 18.8 ± 2.7 211.2 ± 54.9
    AUC(0-∞) (ng/mL*h) 19.1 ± 2.8 227.9 ± 60.1
    MRT(0-t)( h) 3.2 ± 0.4 2.6 ± 0.5
    MRT(0-∞) (h) 3.4 ± 0.5 3.5 ± 0.9
    t1/2z (h) 1.9 ± 0.2 3.8 ± 0.8
    CLz/F (L/h/kg) 266.0 ± 41.3 4.7 ± 1.2
    Vz/F (L/kg) 708.5 ± 79.9 25.9 ± 11.0
    Cmax (ng/mL) 5.3 ± 0.2 169.5 ± 53.5
    Molecular Weight

    610.74

    Formula

    C37H42N2O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=CC=C(C[C@H]2N(C)CCC3=C2C=C(OC)C(OC)=C3)C=C1OC4=CC5=C(C=C4OC)CCN(C)[C@@H]5CC6=CC=C(O)C=C6
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (81.87 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 1.6374 mL 8.1868 mL 16.3736 mL
    5 mM 0.3275 mL 1.6374 mL 3.2747 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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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 (3.41 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.41 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 20 mg/mL (32.75 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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

    Purity: 99.97%

    SDS (479 KB)

    COA (250 KB) HNMR (280 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    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 (protect from light). 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 1.6374 mL 8.1868 mL 16.3736 mL 40.9339 mL
    5 mM 0.3275 mL 1.6374 mL 3.2747 mL 8.1868 mL
    10 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0934 mL
    15 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7289 mL
    20 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
    25 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.6374 mL
    30 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3645 mL
    40 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0233 mL
    50 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
    60 mM 0.0273 mL 0.1364 mL 0.2729 mL 0.6822 mL
    80 mM 0.0205 mL 0.1023 mL 0.2047 mL 0.5117 mL
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    Liensinine 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:

    Liensinine2586-96-1JAKAktAutophagyp38 MAPKReactive Oxygen Species (ROS)VEGFRSTATAmyloid-βHIF/HIF Prolyl-HydroxylaseApoptosisJNKPI3KJanus kinasePKBProtein kinase BVascular endothelial growth factor receptorβ-amyloid peptideAβAbetaHypoxia-inducible factorsHIFsHIF-PHc-Jun N-terminal kinasePhosphoinositide 3-kinaseSTAT3JNK MAPKPI3K/AKT signaling pathwayAMPKHIF-1αMG-63SaOS-2JAK2acetylcholinesteraseInhibitorinhibitorinhibit

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