Oridonin

SKU: orb1225418

Description

Oridonin is an active diterpenoid compound isolated from the plant Rabdosia Rrubescens, has various pharmacological activities, including antioxidant, anti-tumor capacities and anti-inflammation; inhibits AKT kinase activity (AKT1 and AKT2 IC50=8.4 and 8.9 uM) and interacts with the ATP-binding pocket of AKT, inhibits growth of ESCC in vitro and patient derived xenografts in vivo; inhibits vascular inflammation by blocking NF-κB and MAPK activation.

Key Properties

• CAS Number: 28957-04-2
• MW: 364.438
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₈O₆
• SMILES: C=C([C@H](CC1)[C@H]2O)C([C@@]32[C@]4(O)[C@@H](O)[C@]5([H])C(C)(C)CC[C@H](O)[C@@]5(CO4)[C@@]31[H])=O
• Target: Terpenoids
• Solubility: Ethanol: 28 mg/mL (76.83 mM); DMSO: 72 mg/mL (197.57 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Oridonin (160 mg/kg, p.o.) shows significant reduction in the tumor growth without obvious weigh loss in SCID mice bearing EG9 and HEG18 tumor cells. Oridonin treatment also suppresses the expression of Ki-67, phosphorylated AKT, GSK-3β or mTOR in mice. Oridonin (15 mg/kg, i.p.) impairs cell growth in breast cancer with hyperactivation of AKT signaling in nude mice.
• In Vitro:
  Oridonin is an ATP-competitive inhibitor of AKT with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2, respectively. Oridonin (5, 10 or 20 μM) obviously inhibits the growth of KYSE70, KYSE410 and KYSE450 ESCC cells via targeting AKT1/2. Oridonin (10 or 20 μM) causes G2/M phase cell cycle arrest in KYSE70, KYSE410 and KYSE450 cells, and induces apoptosis in these three cell lines at 20 μM. In addition, Oridonin (5, 10 or 20 μM) in combination with cisplatin or 5-FU enhances the inhibition of esophageal squamous cell carcinoma (ESCC) cell growth. Oridonin (0.1 and 1 μM) preferentially suppresses AKT/mTOR signaling. Oridonin (1 μM) also selectively suppresses growth of breast cancer cells with hyperactivation of AKT signaling.

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 250682

Quick Database Links

Gene Symbol

Terpenoids