Withaferin A

SKU: orb1224867

Description

Withaferin A is a steroid lactone that displays anti-inflammatory, antitumor and antiangiogenic activity, potently inhibits NF-κB activation by preventing the TNF-induced activation of IKKβ via a thioalkylation-sensitive redox mechanism; potently inhibits the chymotrypsin-like activity of a purified rabbit 20S proteasome (IC50=4.5 uM) and 26S proteasome in human prostate cancer cultures (at 5-10 uM) and xenografts (4-8 mg/kg/day), inhibits cell proliferation in HUVECs (IC50 =12 nM).(In Vitro):Withaferin A has antiinflammatory activity, and potently inhibits NF-kB activation by preventing the TNF-induced activation of Ik-B kinase beta via a thioalkylation-sensitive redox mechanism. Withaferin A also has anticancer activity. Withaferin A targets the IF protein vimentin, causes aggregation of vimentin filaments in bovine aortic endothelial cells (BAECs) at 3 μM, and induces vimentin fragmentation in endothelial cells at 10 μM. Withaferin A (0.5, 1.5 μM) alone or incombination with cisplatin (CIS) dose-dependently reduces tumorigenic potential of ALDH1 positive cancer stem cells (CSCs).(In Vivo):Withaferin A (2 mg/kg, i.p.) shows potent angiogenesis inhibitory activity via vimentin in mice. Withaferin A (2 mg/kg) combined with cisplatin (CIS) regulates the expression of ALDH1 marker, and downregulates the expression of securin in tumors collected from mice.

Key Properties

• CAS Number: 5119-48-2
• MW: 470.6
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₈O₆
• SMILES: CC12C(CCC2[C@@H](C)[C@H](O)CC(CO3)=C(C)C3=O)C4C[C@@H]5[C@](C6(C)C4CC1)(O5)[C@@H](O)C=CC6=O
• Target: NF-κB
• Solubility: In Vitro: DMSO : 50 mg/mL (106.25 mM)

Bioactivity

• In Vivo:
  Withaferin A (2 mg/kg, i.p.) shows potent angiogenesis inhibitory activity via vimentin in mice. Withaferin A (2 mg/kg) combined with cisplatin (CIS) regulates the expression of ALDH1 marker, and downregulates the expression of securin in tumors collected from mice.
• In Vitro:
  Withaferin A has antiinflammatory activity, and potently inhibits NF-kB activation by preventing the TNF-induced activation of Ik-B kinase beta via a thioalkylation-sensitive redox mechanism. Withaferin A also has anticancer activity. Withaferin A targets the IF protein vimentin, causes aggregation of vimentin filaments in bovine aortic endothelial cells (BAECs) at 3 μM, and induces vimentin fragmentation in endothelial cells at 10 μM. Withaferin A (0.5, 1.5 μM) alone or incombination with cisplatin (CIS) dose-dependently reduces tumorigenic potential of ALDH1 positive cancer stem cells (CSCs).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 101088 | NSC 273757

Quick Database Links

Gene Symbol

NF-κB