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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[1][2][3].

Product Specifications

CAS Number

[29479-00-3]

UNSPSC

12352005

Hazard Statement

H302+H332

Target

Akt; Apoptosis; Caspase; CDK; Cytochrome P450; Interleukin Related; NF-κB; NOD-like Receptor (NLR) ; p38 MAPK; PI3K

Type

Natural Products

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB; PI3K/Akt/mTOR

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/tabersonine-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C(OC)C1=C2NC3=CC=CC=C3[C@@]24CCN5CC=C[C@@]([C@@]45[H])(CC)C1.Cl

Molecular Formula

C21H25ClN2O2

Molecular Weight

372.89

Precautions

P261-P264-P270-P271-P304+P340-P330-P501

References & Citations

[1]Zhang D, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination. Biochem Pharmacol. 2018 Aug;154:183-192.|[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.|[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.

Shipping Conditions

Room temperature

Scientific Category

Natural Products

Clinical Information

No Development Reported

Isoform

Caspase 1; Caspase 8; CDK4; IL-1; NLRP3

Available Sizes

Curated Selection

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