Tabersonine

• Description :

  Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine 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 also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine 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 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].

• CAS Number :

  [4429-63-4]

• UNSPSC :

  12352005

• Hazard Statement :

  H302

• 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 :

  Cancer; Inflammation/Immunology

• Assay Protocol :

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

• Purity :

  98.14

• Solubility :

  DMSO : 25 mg/mL (ultrasonic)

• Smiles :

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

• Molecular Formula :

  C21H24N2O2

• Molecular Weight :

  336.43

• Precautions :

  H302

• 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

• Storage Conditions :

  4°C (Powder, protect from light)

• Scientific Category :

  Natural Products

• Clinical Information :

  No Development Reported

• Isoform :

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