Hispidulin

SKU: orb1296134

Description

Hispidulin is a naturally occurring flavone that acts as a Pim-1 kinase inhibitor with an IC50 of 2.71 µM. It is utilized in biochemical research to study oncology, inflammation, and neuroprotection, with applications in both cell-based assays and animal models.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1447-88-7
• MW: 300.26
• Purity: 97.54% (May vary between batches)
• Formula: C₁₆H₁₂O₆
• SMILES: COc1c(O)cc2oc(cc(=O)c2c1O)-c1ccc(O)cc1
• Target: Pim
• Solubility: DMSO:60 mg/mL (199.83 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.66 mM)

Bioactivity

• Target IC50:
  Pim1:2.71 μM
• In Vivo:
  Hispidulin treatment effectively mitigates ovariectomy-induced body and bone loss while reducing trabecular spacing in mice . When administered intraperitoneally (10 or 50mg/kg) 30 minutes prior to kainic acid injection (15mg/kg), hispidulin increases seizure latency and lowers seizure scores in rats. Furthermore, it significantly reduces hippocampal neuronal cell death caused by kainic acid, an effect paralleled by diminished microglial activation and decreased production of proinflammatory cytokines, including interleukin-1β, interleukin-6, and tumor necrosis factor-α in the hippocampus .
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• In Vitro:
  Hispidulin induces cell death in HepG2 cells in a dose- and time-dependent manner. It promotes apoptosis via mitochondrial dysfunction, characterized by a decreased Bcl-2/Bax ratio, disrupted mitochondrial membrane potential, increased cytochrome C release, and activated caspase-3 .
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• Cell Research:
  HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 μM) for 24, 48 and 72 h. Following treatment, cells are further incubated with MTT reagents at 37°C for 4 h before DMSO is added, to dissolve formazan crystals, and absorbance is measured at 570 nm in a microplate reader .
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• Animal Research:
  The tumor is established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40 mg/kg/day for 35 days. The body weight of tumor-bearing mice is recorded every week and tumor volume is calculated .
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Storage & Handling

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

Alternative Names

Inhibitor, Hispidulin, inhibit, Dinatin, Pim, Pim kinases, Pim1

Compound Identifiers

PubChem CID

5281628