2. Immunology/Inflammation NF-κB MAPK/ERK Pathway Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis PI3K/Akt/mTOR
  3. Akt Interleukin Related NF-κB p38 MAPK CDK NOD-like Receptor (NLR) Caspase Apoptosis Cytochrome P450 PI3K
  4. Tabersonine hydrochloride

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

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CAS No. : 29479-00-3

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Based on 3 publication(s) in Google Scholar

Other Forms of Tabersonine hydrochloride:

Tabersonine hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Tabersonine hydrochloride purchased from MedChemExpress. Usage Cited in: Phytother Res. 2023 Jun;37(6):2353-2363.  [Abstract]

    Tabersonine (Tab; 20 mg/kg; i.v; every 2 days for 12 weeks) significantly reduces the expression and transcription of these fibrotic related biomarkers (mRNA levels of Col1a1, Tgfb1, and Acta2, protein levels of COL-1 and TGF-β) in C57BL/6 mice.

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    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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    NLRP3 NLRP1 NOD1 NOD2

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    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer[1][2][3].

    IC50 & Target

    CDK4

     

    IL-1β

     

    Caspase-1

     

    Caspase-8

     

    NLRP3

     

    In Vitro

    Tabersonine hydrochloride (0.78-25 μM; 24 h) inhibits the cell viability of human liver cancer cells SMMC-7721, HepG2 and human normal liver cells HL-7702, with a stronger inhibitory effect on liver cancer cells[1].
    Tabersonine hydrochloride (6.25-25 μM; 24 h) induces apoptosis of human liver cancer cells SMMC-7721, upregulates the expression of Bax, cleaved-caspase-3, and cleaved-PARP proteins, and downregulates the expression of Bcl-2 protein[1].
    Tabersonine hydrochloride (12.5-25 μM; 24 h) arrests the cell cycle of SMMC-7721 cells at the G0/G1 phase, and downregulates the expression of CDK4 and Cyclin D1 proteins[1].
    Tabersonine hydrochloride (25 μM; 6 h, 12 h, 24 h) inhibits the mRNA and protein expressions of NLRP3, ASC, cleaved-caspase-1, and IL-1β in SMMC-7721 cells[1].
    Tabersonine hydrochloride (6-30 μM; 18 h) induces apoptosis in HepG2 cells, resulting in mitochondrial function impairment, and PI3K/Akt pathway inhibition[2].
    Tabersonine hydrochloride inhibits NLRP3-mediated IL-1β production in BMDM cells with an IC50 of 0.71 μM[3].

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

    Tabersonine hydrochloride Related Antibodies

    Cell Viability Assay[1]

    Cell Line: SMMC-7721, HepG2, HL-7702
    Concentration: 0.78 μM, 1.56 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM
    Incubation Time: 24 h
    Result: Inhibited the cell viability of SMMC-7721, HepG2 and HL-7702 cells. The inhibitory effect on SMMC-7721 and HepG2 cells was stronger than that on HL-7702 cells, indicating a certain degree of selectivity for tumor cells.

    Apoptosis Analysis[1]

    Cell Line: SMMC-7721
    Concentration: 6.25 μM, 12.5 μM, 25 μM
    Incubation Time: 24 h
    Result: Induced apoptosis in SMMC-7721 cells.
    The protein expression of Bax, cleaved-caspase-3 and cleaved-PARP was up-regulated, while the protein expression of Bcl-2 was down-regulated.
    In Vivo

    Tabersonine (10-40 mg/kg; intraperitoneal injection; once a day; 30 days) hydrochloride reduces lung tissue pathological damage, inhibits neutrophil infiltration, reduces MPO activity and TNF-α, IL-6, and IL-1β levels in the mouse LPS-induced acute lung injury model[1].
    Tabersonine (25, 50 mg/kg; oral gavage; once a day; 3 weeks) hydrochloride significantly inhibits tumor growth in the nude mouse HepG2 liver cancer xenograft model, induces the expression of cleaved Caspase-3 in tumor tissues and promotes cell apoptosis[2].
    Tabersonine (10 mg/kg; gavage; 3 times a day; 48-120 h) hydrochloride inhibits NLRP3 inflammasome activation, reduces IL-1β release and inflammatory cell infiltration in the mouse LPS-induced acute lung injury and Alum-induced peritonitis models; and increases the 48-hour survival rate of mice to 60% in the Escherichia coli-induced sepsis model[3].

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

    Animal Model: Male C57BL/6 mice (25-30 g, 8-10 weeks old), LPS-induced acute lung injury model[1]
    Dosage: 10, 20, 40 mg/kg Tabersonine
    Administration: Intraperitoneal injection, daily for 30 days
    Result: Significantly alleviated pathological injury in lung tissues, inhibited neutrophil infiltration, reduced myeloperoxidase (MPO) activity, and decreased the levels of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β compared to the LPS control group
    Molecular Weight

    372.89

    Formula

    C21H25ClN2O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OC)C1=C2NC3=CC=CC=C3[C@@]24CCN5CC=C[C@@]([C@@]45[H])(CC)C1.Cl
    Structure Classification
    Initial Source
    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 : 50 mg/mL (134.09 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 2.6818 mL 13.4088 mL 26.8176 mL
    5 mM 0.5364 mL 2.6818 mL 5.3635 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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    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: ≥ 5 mg/mL (13.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    In Vivo Dissolution Calculator
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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 2.6818 mL 13.4088 mL 26.8176 mL 67.0439 mL
    5 mM 0.5364 mL 2.6818 mL 5.3635 mL 13.4088 mL
    10 mM 0.2682 mL 1.3409 mL 2.6818 mL 6.7044 mL
    15 mM 0.1788 mL 0.8939 mL 1.7878 mL 4.4696 mL
    20 mM 0.1341 mL 0.6704 mL 1.3409 mL 3.3522 mL
    25 mM 0.1073 mL 0.5364 mL 1.0727 mL 2.6818 mL
    30 mM 0.0894 mL 0.4470 mL 0.8939 mL 2.2348 mL
    40 mM 0.0670 mL 0.3352 mL 0.6704 mL 1.6761 mL
    50 mM 0.0536 mL 0.2682 mL 0.5364 mL 1.3409 mL
    60 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1174 mL
    80 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8380 mL
    100 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6704 mL
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    Tabersonine hydrochloride Related Classifications

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    • 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:

    Tabersonine29479-00-3AktInterleukin RelatedNF-κBp38 MAPKCDKNOD-like Receptor (NLR)CaspaseApoptosisCytochrome P450PI3KPKBProtein kinase BILNuclear factor-κBNuclear factor-kappaBCyclin dependent kinaseCYPsPhosphoinositide 3-kinaseAβ(1-42)LI/ARDSInhibitorinhibitorinhibit

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