Apigenin

For research use only.

Catalog No.S2262 Synonyms: NSC 83244, LY 080400

13 publications

Apigenin Chemical Structure

CAS No. 520-36-5

Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

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10mM (1mL in DMSO) EUR 88 In stock
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Selleck's Apigenin has been cited by 13 publications

4 Customer Reviews

  • Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration.

    Int J Clin Exp Pathol, 2014, 7(7):3938-3.. Apigenin purchased from Selleck.

  • SKH-1 mice were subjected to UVB radiation (1000 J/m2 daily, 5 days), or topical apigenin (Api, 5 μmol, in 200 μl vehicle, DMSO: acetone 1:9) was applied 1 h prior to each UVB exposure. Mice were also sham-irradiated and treated with apigenin, and the control group of mice was subjected to sham irradiation and vehicle. 24 h after the final UVB exposure, the mice were euthanized, dorsal skin was harvested, fixed in formalin and paraffin-embedded. (A) Representative Hematoxylin and Eosin (H&E) staining of skin sections (scale bar, 100 μm). (B) Quantitation of epidermal thickness (mean ± SD), *, P < 0.001; **, P< 0.0001. Three sections per mouse and 3 mice per group were evaluated.

    Cell Signal, 2016, 28(5):460-468. Apigenin purchased from Selleck.

  • The effects of apigenin and GLUT-1 AS-ODNs on xenograft apoptosis (the second experiment), observed an under optical microscope (magnification, ×400), and the percentage of apoptotic cells in 100 cells per field was counted and used to calculate the mean apoptosis index (AI). AI, apoptotic index.

    Oncol Rep, 2015, 34(4):1805-14. Apigenin purchased from Selleck.

  • GLUT-1 mRNA expression levels were significantly reduced in the ACC-2 human adenoid cystic carcinoma cells following treatment with increasing doses of apigenin (P<0.05), as determined by reverse transcription-quantitative polymerase chain reaction. Following treatment with 10 µM apigenin, the expression levels of GLUT-1 mRNA did not vary significantly with increasing treatment duration (P>0.05). Following treatment with 40 and 160 µM apigenin, the expression levels of GLUT-1 mRNA were significantly reduced with increasing treatment duration. *P<0.05 vs. control. GLUT-1, glucose transporter-1.

    Mol Med Rep, 2015, 12(5):6461-6. Apigenin purchased from Selleck.

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Biological Activity

Description Apigenin (NSC 83244, LY 080400) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse RAW264.7 cells NEe0eGdHfW6ldHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKEORWEKgdJJwfGWrbjDlfJBz\XO|aX;uJIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|LDDJR|UxRTBwNTFOwG0> NFG4RYgyPjB|OEWzOi=>
human H295R cells NH3jcIRHfW6ldHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGG{b33heIF{\SCneIDy[ZN{\WRiaX6gbJVu[W5iSEK5OXIh[2WubIOsJGlEPTB;MTFOwG0> MUOxPFc4QDl2NB?=
HEK293 FS cells NWrIbHl6TnWwY4Tpc44h[XO|YYm= MoTmTY5pcWKrdHnvckBw\iCQT2i0JIV5eHKnc4Pl[EBqdiCKRVuyPVMhTlNiY3XscJMh[XO|ZYPz[YQh[XNiSELPNkBxem:mdXP0bY9vKGK7IFiyU|IwXHm{L1zQU{Bie3OjeTygTWM2OD1zLkGzJO69VQ>? NHLKSY0zODd|MUO1Oy=>
human HeLa cells NYfGfFJ[TnWwY4Tpc44h[XO|YYm= MonLTY5pcWKrdHnvckBw\iCPUmCxJJRz[W6|ZnXjeIVlKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdM1jdUHREPCC2cnHud5BwenRiYomgdoFxcWRiZnnseJJifGmxbjDhd5NigSxiS3m9Nk41KM7:TR?= MXixPVczPTV5OB?=
human MV4-11 cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= MVW3NkBp MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMhcGG{Yn;ybY5oKE[OVEOgcZV1[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IITleJJigm:uaYXtJIJie2WmIFX6JGN6XG:6IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBIUTVyPUKuPFEh|ryP M2Pq[|I{PDFzMEez
human mast cells NF3YOWFHfW6ldHnvckBie3OjeR?= Mnu4TY5pcWKrdHnvckBw\iCVWVugbY4hcHWvYX6gcYF{fCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gcYF{fCClZXzsJIRm\3KjboXsZZRqd25uIFXDOVA:OyEQvF2= NWW4dW5oOjF|NUS4NFA>
MDCK cells M{\QXGZ2dmO2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2GQ1ugZ4VtdHNidYPpcochUG:nY3jzeEA{OzN2MjDzeIFqdmmwZzygTWM2OD1|LkGg{txO M2O2OlIyOzV2OECw
human MDA-kb2 cells MV;GeY5kfGmxbjDhd5NigQ>? NF3jXnZCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIF3ERU1s[jJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFUFRvaX7keYNm\CCudXPp[oVz[XOnIHHjeIl3cXS7IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF02NjJizszN M{f5W|E6PTl{MkS1
MCF-7 MX cells MoTySpVv[3Srb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2FRj23JG1ZKGOnbHzzJJV{cW6pIFjv[YNpe3RiM{OzOFIhe3SjaX7pcoctKEmFNUC9OU46KM7:TR?= M1f1dFIyOzV2OECw
mouse RAW264.7 cells MYPGeY5kfGmxbjDhd5NigQ>? MlvtNlQhcA>? MUPBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHnZYlve3RibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBvcXS{aYTlJIFk[3WvdXzheIlwdiCjZoTldkAzPCCqcoOgZpkhT3KrZYPzJJJm[WenboSgcYV1cG:mLDDJR|UxRTZwNzFOwG0> NYm4[4tjOTl5N{iwPFY>
human H9 cells NUDxcVlzTnWwY4Tpc44h[XO|YYm= NXjFe5ViOyCmYYnz MWXBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIFi5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhOyCmYYnzJIJ6KHB{NDDhcpRq\2WwIHPhdJR2emViYYPzZZktKEWFNUC9PUDPxE1? NF;BZ|I5OTV6MU[0
HEK293 cells NY\0XItiTnWwY4Tpc44h[XO|YYm= M4DXNlI1KGh? NUfWc45CSWexbnnzeEBi[3Srdnn0fUBifCCvb4Xz[UBRWEGUZ3HtcYEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bkdy2neIDy[ZN{cW6pIIfpeIghT2GuNDDy[ZBwenSncjD2[YN1d3JiYX\0[ZIhOjRiaILzJIJ6KGS3YXytcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygSWM2OD1{ND65JO69VQ>? NI\xOmgzPDl3NUi4PS=>
mouse 26-L5 cells NVvXdYpQWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml7NO|IhcA>? M1X3cGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViMk[tUFUh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1{NTFOwG0> MVSxNlAzPzd|OR?=
human RS4:11 cells NWewdoJsS3m2b4TvfIlkcXS7IHHzd4F6 M4TK[VczKGh? MmHVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnM1QjFzIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViRlzUN{Bi\nSncjC3NkBpenNiYomgeIV1emG8b3zpeY0h[mG|ZXSgSZohS3mWb4igZ4VtdCC4aXHibYxqfHliYYPzZZktKEeLNUC9NlcvQSEQvF2= MWCyN|QyOTB5Mx?=
mouse B16-BL6 cells MnmzVJJwdGmoZYLheIlwdiCjc4PhfS=> NH64bZY4OiCq MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEJzNj3CUFYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1|MT62JO69VQ>? M1XqcVEzODJ5N{O5
human H9 cells NWLqSIwxS3m2b4TvfIlkcXS7IHHzd4F6 NILHcY0{KGSjeYO= NHz0enpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJQSClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OzVizszN NUDheGl{QDF3OEG2OC=>
human HT1080 cells M4HlT3Bzd2yrZnXyZZRqd25iYYPzZZk> MYS3NkBp M3nUUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSxNFgxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlE MWSxNlAzPzd|OR?=
MDCK cells MlnlR5l1d3SxeHnjbZR6KGG|c3H5 MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{KGK7IF3UWEBie3OjeTygR2M2OD1|OT61PUDPxE1? MYixPFY1ODB2Mh?=
mouse L929 cells Mn3iSpVv[3Srb36gZZN{[Xl? NV7FZ3lmOTVibXnudy=> NH;CSmNRd3SnboTpZZRqd25ib3[gdoVkd22kaX7hcpQhcHWvYX6gWG5HNWGucHjhMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KG:oIH3veZNmKEx7MkmgZ4VtdHNiYYPz[ZN{\WRiYYOgd5Vzfmm4YXzpeJkheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIJm\m:{ZTDUUmZidHCqYTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB{NDDodpMh[nliY4L5d5RidCC4aX;s[ZQhe3SjaX7pcoc> NX3uPId[QTJ6N{SxOS=>
human THP1 cells MVjGeY5kfGmxbjDhd5NigQ>? MXGyNEB2VQ>? NYD1R4toOSCq Mk\4TY5pcWKrdHnvckBw\iCQT2iyJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZiVGDBMYlv\HWlZXSgR2Q{PiCvUl7BJIV5eHKnc4Ppc44h[XRiMkCgeW0hcW6ldXLheIVlKG[xcjCxJIhzKHC{aX;yJJRwKFSSQTDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? MYmyN|c5PjV{MB?=
MDA-MB-231 cells M1XiUGZ2dmO2aX;uJIF{e2G7 NGe1T2c2KHWP NYPhUHN5UW6qaXLpeIlwdiCxZjDQUWEue3SrbYXsZZRm\CCQRj3rZZBx[UJic3nncoFtcW6pIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPSC3TTDpcoN2[mG2ZXSg[o9zKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= M1KzWVI2OTlyNE[2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MHC / MHC2A / MHC2B / MyoD ; 

PubMed: 29108230     


Apigenin increases total MHC, MHC2A, MHC2B and myoD expression in C2C12 cells. 

CXCR4; 

PubMed: 23743303     


(C) Apigenin suppressed CXCR4 levels in a dose-dependent manner. Cells were treated with the indicated concentrations of apigenin for 24 hours. CXCR4 expressions were indicated by anti-CXCR4 and anti-GAPDH western blotting analyses. (D) Apigenin suppressed CXCR4 levels in a time-dependent manner. Cells were treated with 40 μM apigenin for the indicated times, after which western blotting was performed as described above.

CDK1 / Cyclin B1 / p21 ; 

PubMed: 24009741     


Immunoblot analysis of G2/M phase regulators in cells treated with apigenin for 24 hr. CT: control.

29108230 23743303 24009741
Immunofluorescence
E-caherin / Vimentin ; 

PubMed: 27203387     


Typical images of immunofluorescent double staining for E-cadherin and Vimentin in Bel-7402 and PLC/PRF/5 cells. Each experiment was performed in triplicate.

Snail; 

PubMed: 27203387     


Typical immunofluorescence images of Snail in Bel-7402 and PLC/PRF/5 cells. Each experiment was performed in triplicate.

27203387
Growth inhibition assay
Cell viability; 

PubMed: 23224239     


Effect of apigenin on cell viability. Cells were treated with various concentrations of apigenin (2–30 μg/ml) for 24 h and cell viability was measured by MTT assay. Statistical significance: *p < 0.001.

23224239
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]

Protocol

Cell Research:

[5]

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  • 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.


    (Only for Reference)
Animal Research:

[6]

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  • Animal Models: heterozygous C57BL/TGN TRAMP mice
  • Dosages: 20 and 50 μg/mouse/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (199.82 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 270.24
Formula

C15H10O5

CAS No. 520-36-5
Storage powder
in solvent
Synonyms NSC 83244, LY 080400
Smiles C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID