Apigenin

SKU: orb1306215

Description

Apigenin is a naturally occurring flavonoid and a competitive CYP2C9 inhibitor (Ki=2 μM). It is widely used in research to study its anxiolytic, immunomodulatory, and sedative properties, with applications in both in vitro enzyme assays and in vivo pharmacological models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 520-36-5
• MW: 270.24
• Purity: 99.66% (May vary between batches)
• Formula: C₁₅H₁₀O₅
• SMILES: OC1=CC=C(C=C1)C1=CC(=O)C2=C(O)C=C(O)C=C2O1
• Target: Cytochromes P450,Autophagy,Endogenous Metabolite
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:255 mg/mL (943.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (18.5 mM)

Bioactivity

• Target IC50:
  CYP2C9:2 μM (Ki)|Microsomes (Rat):25.73 μM|Microsomes (human):58.37 μM
• In Vivo:
  Apigenin at a dosage of 12.5 mg/kg enhances the proliferation of cells in the dentate gyrus region of the hippocampus in adult mice. It also downregulates the production of IL-4 in ovalbumin-immunized BALB/C mice. Additionally, apigenin significantly increases both the weight of the uterus and the overall concentration of estrogen receptor (ER)-α in female mice (64), while inhibiting the growth of prostate and breast cancer cells via the estrogen receptor β1. This compound inhibits lung metastasis of melanoma by blocking the interaction between tumor cells and endothelial cells. Furthermore, apigenin reduces IGF-I levels in prostate xenografts and increases the content of IGFBP-3, a protein that binds IGF-I in the bloodstream.
• In Vitro:
  Apigenin inhibits the activity of protein kinase C, mitogen-activated protein kinase, and the transformation of C3HI mouse embryo fibroblasts, as well as downstream oncogenes in NIH3T3 cells transformed by v-Ha-ras. It also suppresses the activity and expression of cyclooxygenase-2 and nitric oxide synthase-2 in mouse macrophages induced by LPS and effectively blocks the upregulation of the cell adhesion molecule-1 in human endothelial cells triggered by TNFα. Moreover, apigenin inhibits the expression of HIF-1α and VEGF in human ovarian cancer cells through the PI3K/Akt/p70S6K1 and HDM2/p53 signaling pathways, reduces the phosphorylation levels of cellular proteins induced by TPA, and inhibits the expression of c-jun and c-fos also induced by TPA. It reverses the transformed phenotype of NIH3T3 cells with v-H-ras. In Chinese hamster ovary cells, apigenin prevents mutations caused by the toxicity gene induced by nitropyrene. It blocks the peroxisome proliferator-activated kinase and MAPK in hepatocytes ex vivo. In epithelial and fibroblast cells, apigenin causes reversible blocks at G2/M and G0/G1 phases by inhibiting p34 (cdc2) kinase activity, accompanied by an increase in p53 protein stability.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, NSC 83244, LY080400, LY-080400, LY 080400, NSC83244, NSC-83244, Inhibitor, 4',5,7-Trihydroxyflavone, Apigenol, Apigenin, Autophagy, C.I. Natural Yellow 1, CYP2C9, CYPs, Cytochrome P450

Compound Identifiers

PubChem CID

5280443

Sang A Kwak 1, Jane J Lee 1, Ju Hong Park 2, Nami Joo 1 Phytochemical Profiling and Anti-Inflammatory Effects of Aerial and Underground Parts of Apium graveolens var. rapaceum (Celeriac): Potential Health Benefits of Discarded Aerial Parts Food Sci Nutr, (2025)

PubMed: 41049417