Home Metabolism P450 (e.g. CYP17) inhibitor Apigenin For research use only.

Apigenin

Synonyms: LY 080400, NSC 83244

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

Apigenin Chemical Structure

Apigenin Chemical Structure

CAS No. 520-36-5

Purity & Quality Control

Apigenin Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse RAW264.7 cells Function assay Inhibition of COX2 protein expression in mouse RAW264.7 cells, IC50=0.5 μM 16038536
human H295R cells Function assay Inhibition of aromatase expressed in human H295R cells, IC50=1 μM 18778944
HEK293 FS cells Function assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.13 μM 20731357
human HeLa cells Function assay Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM 19725578
human MV4-11 cells Cytotoxicity assay 72 h Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=2.81 μM 23411073
human mast cells Function assay Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=3 μM 21354800
MDCK cells Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=3.1 μM 21354800
human MDA-kb2 cells Function assay Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=5.2 μM 19592245
MCF-7 MX cells Function assay Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=5.9 μM 21354800
mouse RAW264.7 cells Function assay 24 h Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method, IC50=6.7 μM 19778086
human H9 cells Function assay 3 days Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=9 μM 8158164
HEK293 cells Function assay 24 h Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=24.9 μM 24955889
mouse 26-L5 cells Proliferation assay 72 h Antiproliferative activity against mouse 26-L5 cells after 72 hrs by MTT assay, EC50=25 μM 12027739
human RS4:11 cells Cytotoxicity assay 72 h Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=27.9 μM 23411073
mouse B16-BL6 cells Proliferation assay 72 h Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay, EC50=31.6 μM 12027739
human H9 cells Cytotoxicity assay 3 days Cytotoxicity against human H9 cells after 3 days, IC50=35 μM 8158164
human HT1080 cells Proliferation assay 72 h Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay, IC 12027739
MDCK cells Cytotoxicity assay Cytotoxicity against MDCK cells by MTT assay, CC50=39.59 μM 18640042
mouse L929 cells Function assay 15 mins Potentiation of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining 9287415
human THP1 cells Function assay 20 uM 1 h Inhibition of NOX2 in human THP1 cells assessed as downregulation of TPA-induced CD36 mRNA expression at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis 23786520
MDA-MB-231 cells Function assay 5 uM Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay 25190466
Click to View More Cell Line Experimental Data

Biological Activity

Description Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
Features Much more potent than kaempferol and myricetin in CT-L inhibition.
Targets
CYP2C9 [5]
2 μM(Ki)
In vitro
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot MHC / MHC2A / MHC2B / MyoD CXCR4 CDK1 / Cyclin B1 / p21 29108230
Immunofluorescence E-caherin / Vimentin Snail 27203387
Growth inhibition assay Cell viability 23224239
In Vivo
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]
Animal Research Animal Models heterozygous C57BL/TGN TRAMP mice
Dosages 20 and 50 μg/mouse/day
Administration p.o.

Chemical Information & Solubility

Molecular Weight 270.24 Formula

C15H10O5

CAS No. 520-36-5 SDF Download Apigenin SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (199.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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