Drug intelligence / Profile preview

celastrol

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
01

Overview

Celastrol is a pentacyclic triterpenoid compound isolated from the root extracts of Tripterygium wilfordii (Thunder God Vine), a traditional Chinese medicinal plant[1][2][6]. It exhibits potent anti-inflammatory, antioxidant, and anticancer activities. Celastrol has demonstrated neuroprotective effects in preclinical models of memory impairment and neurodegenerative diseases by reducing oxidative stress and attenuating neuroinflammation[1][2]. Its mechanisms include modulation of multiple cell signaling pathways such as NF-κB, MAPK, JAK/STAT, PI3K/Akt/mTOR pathways; inhibition of angiogenesis via VEGFR suppression; regulation of apoptosis and proteasome activity; stimulation of heat-shock protein response; immunomodulation; and leptin sensitization for potential obesity treatment[2][6]. Celastrol is being explored as a lead molecule for drug development targeting chronic inflammatory diseases (e.g., rheumatoid arthritis), autoimmune disorders (e.g., systemic lupus erythematosus), neurodegenerative conditions (e.g., Alzheimer's disease), cancer, obesity/metabolic syndrome, type 2 diabetes mellitus and more[1][2].

Other names
去水卫矛醇tripterinecelastrocelasterolcelatrol
02

Targets

MEKMYC (MYC proto-oncogene protein)

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