| Name | Hispidulin |
| Description | Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM). |
| 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 [2]. |
| 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 [2]. |
| 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 [2]. |
| In vivo | Hispidulin treatment effectively mitigates ovariectomy-induced body and bone loss while reducing trabecular spacing in mice [3]. 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 [4]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : Insoluble
DMSO : 60 mg/mL (199.83 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.66 mM), Sonication is recommended.
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| Keywords | Pim1 | Pim kinases | Pim | Inhibitor | inhibit | Hispidulin |
| Inhibitors Related | Pim1/AKK1-IN-1 | TCS-PIM-1-4a | SGI-1776 | CK2/ERK8-IN-1 | M-110 | NSC756093 | Pim-1 kinase inhibitor 4 | AZD1208 | Pim-1/2 kinase inhibitor 1 | Pim-1 kinase inhibitor 8 | TP-3654 | K00135 |
| Related Compound Libraries | Anti-Tumor Natural Product Library | Flavonoid Natural Product Library | Traditional Chinese Medicine Monomer Library | Bioactive Compound Library | Natural Product Library | Anti-Inflammatory Traditional Chinese Medicine Compound Library | Miao medicine Compound Library | Natural Product Library for HTS | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Heat-Clearing and Detoxifying Traditional Chinese Medicine Compound Library | Food as Medicine Compound Library |
United States
