Hellebrigenin

SKU: orb1684551

Description

Hellebrigenin is a small molecule that inhibits MAPK pathways (ERK, p38, JNK) and XIAP, downregulating Akt and inducing apoptosis via caspase activation and DNA damage. It demonstrates anti-proliferative effects in research models of oral squamous cell carcinoma and liver cancer, both in vitro and in vivo.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 465-90-7
• MW: 416.51
• Purity: 99.98% (May vary between batches)
• Formula: C₂₄H₃₂O₆
• SMILES: C(=O)[C@@]12[C@@]3([C@]([C@]4(O)[C@](C)(CC3)[C@H](CC4)C=5C=CC(=O)OC5)(CC[C@]1(O)C[C@@H](O)CC2)[H])[H]
• Target: IAP,JNK,p38 MAPK,PARP,ERK,Apoptosis,Caspase

Bioactivity

• In Vivo:
  Methods: Hellebrigenin (6 mg/kg, intraperitoneal injection, three times a week for 4 weeks) was used to treat oral cancer SCC-1 cell xenograft model mice to study its effects on tumor growth and mouse body weight. Methods: Hellebrigenin significantly inhibited tumor growth in the oral cancer SCC-1 cell xenograft model of mice without affecting mouse body weight.
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• In Vitro:
  Methods: Oral cancer SCC-1/47 cells and liver cancer HepG2 cells were treated with Hellebrigenin (2-8 nM, 24-72 h), and cell viability was detected by MTT assay. Results: Hellebrigenin inhibited the cell viability of oral cancer SCC-1/47 cells and liver cancer HepG2 cells in a dose- and time-dependent manner. Methods: Oral cancer SCC-1/47 cells were treated with Hellebrigenin (2-8 nM, 24 h), and the expression of related apoptosis proteins was detected by WB. Results: Hellebrigenin induced apoptosis in oral cancer SCC-1/47 cells and activated Caspase-3/8/9 and PARP cleavage, accompanied by upregulation of Bax/Bak and downregulation of Bcl-2/Bcl-xL, Cyclin A2/B1, and CDK4/6.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK, Akt, PARP, Hellebrigenin

Compound Identifiers

PubChem CID

259577