Apigenin

Catalog No.S2262 Batch:S226205

Technical Data

Formula	C₁₅H₁₀O₅
Molecular Weight	270.24	CAS No.	520-36-5
Solubility (25°C)*	In vitro	DMSO	54 mg/mL (199.82 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Apigenin is a potent P450 inhibitor for CYP2C9 with K_i of 2 μM.

Targets

CYP2C9 ^[5]

2 μM(Ki)

In vitro

Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). Apigenin also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. Apigenin exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. ^[1] Apigenin has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. Apigenin suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. Apigenin has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. Apigenin blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. Apigenin has further been shown to down-regulate the expression of the Na⁺/Ca²⁺-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. Apigenin induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. Apigenin is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. Apigenin inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. ^[2] Apigenin inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. Apigenin also inhibits proliferating of human keratinocytes. ^[3]

In vivo

Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. Apigenin inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. Apigenin is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. Apigenin suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. ^[2] Apigenin (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice. ^[4]

Features

Much more potent than kaempferol and myricetin in CT-L inhibition.

Protocol (from reference)

Cell Assay:^{^[5]}	Cell lines WI-38, T-24, HT-1376 and PC-3 cells Concentrations 0, 1, 5, 10, 20, 30, 40, and 50 μg/ml Incubation Time 24 h Method To measure the effect of apigenin on cell viability, the WI-38, T-24, HT-1376 and PC-3 cells were seeded in 24-well plates (1 × 10⁵ cells/well) for 16-18 h. The cells were then treated with or without various concentrations (0, 1, 5, 10, 20, 30, 40, and 50 μg/ml) of apigenin for 24 h. Each treatment was repeated 3 times. After the exposure period, the medium was removed and followed by washing the cells with PBS. The medium was then changed and incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/ml)/well for 4 h. The medium was removed, and formazan was solubilised in isopropanol and measured spectrophotometrically at 563 nm. The percentage of viable cells was estimated by comparing them with the untreated control cells.
Animal Study:^{^[6]}	Animal Models heterozygous C57BL/TGN TRAMP mice Dosages 20 and 50 μg/mouse/day Administration p.o.

Cell Assay:^{^[5]}

Cell lines
WI-38, T-24, HT-1376 and PC-3 cells
Concentrations
0, 1, 5, 10, 20, 30, 40, and 50 μg/ml
Incubation Time
24 h
Method
To measure the effect of apigenin on cell viability, the WI-38, T-24, HT-1376 and PC-3 cells were seeded in 24-well plates (1 × 10⁵ cells/well) for 16-18 h. The cells were then treated with or without various concentrations (0, 1, 5, 10, 20, 30, 40, and 50 μg/ml) of apigenin for 24 h. Each treatment was repeated 3 times. After the exposure period, the medium was removed and followed by washing the cells with PBS. The medium was then changed and incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/ml)/well for 4 h. The medium was removed, and formazan was solubilised in isopropanol and measured spectrophotometrically at 563 nm. The percentage of viable cells was estimated by comparing them with the untreated control cells.

Animal Study:^{^[6]}

Animal Models
heterozygous C57BL/TGN TRAMP mice
Dosages
20 and 50 μg/mouse/day
Administration
p.o.

References

+ Expand

Customer Product Validation

: , , Int J Clin Exp Pathol, 2014, 7(7):3938-3.

: Data from [Data independently produced by , , Cell Signal, 2016, 28(5):460-468]

: Data from [Data independently produced by , , Oncol Rep, 2015, 34(4):1805-14]

: Data from [Data independently produced by , , Mol Med Rep, 2015, 12(5):6461-6]

Selleck's Apigenin has been cited by 29 publications

Connexin43 is associated with the progression of clear cell renal carcinoma and is regulated by tangeretin to sygergize with tyrosine kinase inhibitors [ Transl Oncol, 2023, 35:101712]	PubMed: 37354638
Synergism Antiproliferative Effects of Apigenin and Naringenin in NSCLC Cells [ Molecules, 2023, 28(13)4947]	PubMed: 37446609
Nao Tan Qing ameliorates Alzheimer's disease-like pathology by regulating glycolipid metabolism and neuroinflammation: A network pharmacology analysis and biological validation [ Pharmacol Res, 2022, 185:106489]	PubMed: 36228869
Glycosylated modification of MUC1 maybe a new target to promote drug sensitivity and efficacy for breast cancer chemotherapy [ Cell Death Dis, 2022, 13(8):708]	PubMed: 35970845
Apigenin Induced Apoptosis by Downregulating Sulfiredoxin Expression in Cutaneous Squamous Cell Carcinoma [ Oxid Med Cell Longev, 2022, 2022:8172866]	PubMed: 35965686
Identification of EZH2 as Cancer Stem Cell Marker in Clear Cell Renal Cell Carcinoma and the Anti-Tumor Effect of Epigallocatechin-3-Gallate -EGCG [ Cancers -Basel, 2022, 14-174200]	PubMed: 36077742
Biphasic Effect of Pirfenidone on Angiogenesis [ Chem Biol Interact, 2022, S0009-2797(22)00171-5]	PubMed: 35513012
Novel CFTR modulator combinations maximise rescue of G85E and N1303K in rectal organoids [ ERJ Open Res, 2022, 8(2)00716-2021]	PubMed: 35449760
CDK6 is upregulated and may be a potential therapeutic target in enzalutamide-resistant castration-resistant prostate cancer [ Eur J Med Res, 2022, 27(1):105]	PubMed: 35780240
Apigenin alleviates cancer drug Sorafenib induced multiple toxic effects in Swiss albino mice via anti-oxidative stress [ Toxicol Appl Pharmacol, 2022, 447:116072]	PubMed: 35613639

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SHIPPING AND STORAGE
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