Tabersonine hydrochloride
Based on 3 publication(s) in Google Scholar
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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- Purity: 98.55%
- CAS No.: 29479-00-3
- 화학식: C21H25ClN2O2
- 분자량:372.89
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tabersonine hydrochloride
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Customer Validation & Images
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IHC
All Caspase Isoforms
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Biological Activity
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CDK4 |
IL-1β |
Caspase-1 |
Caspase-8 |
NLRP3 |
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.
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Cell Line:SMMC-7721, HepG2, HL-7702
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Concentration:0.78 μM, 1.56 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM
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Incubation Time:24 h
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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.
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Cell Line:SMMC-7721
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Concentration:6.25 μM, 12.5 μM, 25 μM
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Incubation Time:24 h
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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.
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.
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Animal Model:Male C57BL/6 mice (25-30 g, 8-10 weeks old), LPS-induced acute lung injury model[1]
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Dosage:10, 20, 40 mg/kg Tabersonine
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Administration:Intraperitoneal injection, daily for 30 days
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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
Chemical Information
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CAS No. 29479-00-3
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Appearance Solid
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분자량 372.89
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화학식 C21H25ClN2O2
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Color White to off-white
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SMILES
O=C(OC)C1=C2NC3=CC=CC=C3[C@@]24CCN5CC=C[C@@]([C@@]45[H])(CC)C1.Cl
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Phytother Res
Tabersonine attenuates obesity-induced renal injury via inhibiting NF-κB-mediated inflammation. [Abstract]2023 Jun;37(6):2353-2363. PMID: 36752025
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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Sci Rep
Tabersonine inhibits inflammation and apoptosis through the JAK1/STAT3 signaling pathway to alleviate LPS-induced acute lung injury. [Abstract]2025 Sep 25;15(1):32764. PMID: 40998926
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhang D, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination. Biochem Pharmacol. 2018 Aug;154:183-192. [Content Brief]
[2]. Li X, et al. Tabersonine Induces the Apoptosis of Human Hepatocellular Carcinoma In vitro and In vivo. Anticancer Agents Med Chem. 2024;24(10):764-772. [Content Brief]
[3]. Xu HW, et al. Tabersonine, a natural NLRP3 inhibitor, suppresses inflammasome activation in macrophages and attenuate NLRP3-driven diseases in mice. Acta Pharmacol Sin. 2023 Jun;44(6):1252-1261. [Content Brief]
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 |
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| 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 |
Tabersonine hydrochloride Related Classifications
HY-N1431A Related Classifications
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