Cat. No.: HY-N1431A

Tabersonine hydrochloride

3 Cited Publications

Customer Review

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.

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

Purity: 98.55%
CAS No.: 29479-00-3
Formula: C₂₁H₂₅ClN₂O₂
Molecular Weight:372.89

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tabersonine hydrochloride Chemical Structure

CAS No.: 29479-00-3

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

CDK4

IL-1β

Caspase-1

Caspase-8

NLRP3

All NOD-like Receptor (NLR) Isoforms :

All NF-κB Isoforms :

All CDK Isoforms :

All p38 MAPK Isoforms :

All Cytochrome P450 Isoforms :

All Akt Isoforms :

All Interleukin Related Isoforms :

All PI3K Isoforms :

All Caspase Isoforms :

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.

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

Chemical Information

CAS No. 29479-00-3
Appearance Solid
Molecular Weight 372.89
Formula C₂₁H₂₅ClN₂O₂
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
- Alkaloids
- Indole Alkaloids
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

Publications (3)

All IHC

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Journal Impact Factor

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.
Ind Crops Prod

2025 Aug.
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

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6818 mL

13.4088 mL

26.8176 mL

5 mM

0.5364 mL

2.6818 mL

5.3635 mL

10 mM

0.2682 mL

1.3409 mL

2.6818 mL

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.

Molarity Calculator

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Tabersonine hydrochloride

3 Cited Publications

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Tabersonine hydrochloride

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

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Publications Citing Use of MedChemExpress (MCE) Tabersonine hydrochloride

All NOD-like Receptor (NLR) Isoforms

All NF-κB Isoforms