Terpenoids

Celastrol, a triterpenoid compound isolated from the root bark of the Chinese medicinal plant Tripterygium wilfordii, is known for its antitumor and anti-inflammatory properties but its mode of action and spectrum of cellular targets are poorly understood.

Celastrol was recently found to be a potent inhibitor of the heat-shock protein Hsp90 inducing the disruption of protein-protein interactions of Hsp90 and its co-chaperones [1, 2].

Furthermore, it was shown to act as an effective inhibitor of the transcription factor NF-κB potentiating the apoptosis induced by TNF-α and chemotherapeutic agents and inhibiting invasion [3]. 

1. Zhang T. et al., 2008. A novel Hsp90 inhibitor to disrupt Hsp90/Cdc37 complex against pancreatic cancer cells. Mol. Cancer Ther.; 7: 162-170.
2. Hieronymus H. et al., 2006. Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Cancer Cell. ;10(4):321-30.
3. Sethi G. et al., 2007. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kB–regulated gene products and TAK1-mediated NF-B activation. Blood, 109: 2727 - 2735.

Formula: C₂₉H₃₈O₄
Molecular weight: 450.61 

Celastrol is provided as red cubic crystals. Product is shipped at room temperature.
Store at -20°C. Celastrol is stable for 2 years.

Triptolide, a diterpenoid isolated from the Chinese herb Tripterygium wilfordii hook F, has been used for centuries in traditional Chinese medicine to treat immune-related disorders.

In addition to its anti-inflammatory and immunosuppressive activities, triptolide possesses potent anti-tumor properties. It was shown to suppress the growth and induce apoptosis of a broad range of human tumor cells.

However, despite the recognized potent antitumor activity of triptolide, current knowledge regarding its mechanism of action is still limited. So far, triptolide is known to inhibit the heat shock response [1], block the activation of NF-κB [2] and induce caspase activation [3].

1. Westerheide SD. et al., 2006. Triptolide, an Inhibitor of the Human Heat Shock Response That Enhances Stress-induced Cell Death. J. Biol. Chem., 281: 9616 - 9622.
2. Lee KY. et al., 1999. PG490 (triptolide) cooperates with tumor necrosis factoralpha to induce apoptosis in tumor cells. J Biol Chem. 274: 13451-13455.
3. Bing ZC. et al., 2006. Triptolide induces caspase-dependent cell death mediated via the mitochondrial pathway in leukemic cells. Blood 108: 630 - 637.

Formula: C₂₀H₂₄O₆
Molecular weight: 360.40

Triptolide is provided as a white solid. Product is shipped at room temperature.
Keep away from light at -20°C for long term storage.