Apigenin

Catalog No.S2262 Synonyms: NSC 83244, LY 080400

Apigenin Chemical Structure

Molecular Weight(MW): 270.24

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

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In DMSO USD 90 In stock
USD 70 In stock
USD 120 In stock
USD 210 In stock
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Cited by 6 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.

Purity & Quality Control

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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

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 M4XLZWZ2dmO2aX;uJIF{e2G7 NXu2em1zUW6qaXLpeIlwdiCxZjDDU3gzKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{whUUN3ME2wMlUh|ryP M1TWRVE3ODN6NUO2
human H295R cells NF;pdJFHfW6ldHnvckBie3OjeR?= MoK2TY5pcWKrdHnvckBw\iCjcn;tZZRie2ViZYjwdoV{e2WmIHnuJIh2dWGwIFiyPVVTKGOnbHzzMEBKSzVyPUGg{txO M2nPc|E5Pzd6OUS0
HEK293 FS cells MULGeY5kfGmxbjDhd5NigQ>? MnzJTY5pcWKrdHnvckBw\iCQT2i0JIV5eHKnc4Pl[EBqdiCKRVuyPVMhTlNiY3XscJMh[XO|ZYPz[YQh[XNiSELPNkBxem:mdXP0bY9vKGK7IFiyU|IwXHm{L1zQU{Bie3OjeTygTWM2OD1zLkGzJO69VQ>? NVmyd2tMOjB5M{GzOVc>
human HeLa cells M13se2Z2dmO2aX;uJIF{e2G7 M1LBPGlvcGmkaYTpc44hd2ZiTWLQNUB1emGwc3\lZ5Rm\CCrbjDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{PIYWxVSzRidILhcpNxd3K2IHL5JJJieGmmIH\pcJRz[XSrb36gZZN{[XluIFvpQVIvPCEQvF2= MlrtNVk4OjV3N{i=
human MV4-11 cells M3jyWmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYC3NkBp MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMhcGG{Yn;ybY5oKE[OVEOgcZV1[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IITleJJigm:uaYXtJIJie2WmIFX6JGN6XG:6IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBIUTVyPUKuPFEh|ryP NYX6R5k3OjN2MUGwO|M>
human mast cells MlnrSpVv[3Srb36gZZN{[Xl? NXzROZA2UW6qaXLpeIlwdiCxZjDTXWshcW5iaIXtZY4hdWG|dDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hdWG|dDDj[YxtKGSnZ4LhcpVt[XSrb36sJGVEPTB;MzFOwG0> MoXxNlE{PTR6MEC=
MDCK cells M2PKTGZ2dmO2aX;uJIF{e2G7 NEDUNZFKdmirYnn0bY9vKG:oIFLDVnAh\XiycnXzd4VlKGmwIF3ER2sh[2WubIOgeZNqdmdiSH;lZ4h{fCB|M{O0NkB{fGGrbnnu[{whUUN3ME2zMlEh|ryP MU[yNVM2PDhyMB?=
human MDA-kb2 cells NVr0SXN[TnWwY4Tpc44h[XO|YYm= NIfrcG5CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIF3ERU1s[jJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFUFRvaX7keYNm\CCudXPp[oVz[XOnIHHjeIl3cXS7IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF02NjJizszN NHfnOZcyQTV7MkK0OS=>
MCF-7 MX cells NV;zeHc1TnWwY4Tpc44h[XO|YYm= MnezTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EBqdiCPQ1[tO{BOYCClZXzsd{B2e2mwZzDIc4VkcHO2IEOzN|QzKHO2YXnubY5oNCCLQ{WwQVUvQSEQvF2= MkfBNlE{PTR6MEC=
mouse RAW264.7 cells MXvGeY5kfGmxbjDhd5NigQ>? MWWyOEBp NXHtUGFqSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRibnn0dol1\SCjY3P1cZVt[XSrb36gZYZ1\XJiMkSgbJJ{KGK7IFfybYV{eyC{ZXHn[Y51KG2ndHjv[EwhUUN3ME22Mlch|ryP M1XPZlE6Pzd6MEi2
human H9 cells MlraSpVv[3Srb36gZZN{[Xl? MWezJIRigXN? NXLLT2VFSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBJQSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqemGuIILldIxq[2G2aX;uJIFnfGW{IEOg[IF6eyCkeTDwNlQh[W62aXflckBk[XC2dYLlJIF{e2G7LDDFR|UxRTlizszN NWD4VIFkQDF3OEG2OC=>
HEK293 cells NXrxN3N6TnWwY4Tpc44h[XO|YYm= NHrzcoUzPCCq NYT5ZYQ3SWexbnnzeEBi[3Srdnn0fUBifCCvb4Xz[UBRWEGUZ3HtcYEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bkdy2neIDy[ZN{cW6pIIfpeIghT2GuNDDy[ZBwenSncjD2[YN1d3JiYX\0[ZIhOjRiaILzJIJ6KGS3YXytcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygSWM2OD1{ND65JO69VQ>? NXH6W4d2OjR7NUW4PFk>
mouse 26-L5 cells NGTMepVRem:uaX\ldoF1cW:wIHHzd4F6 NVXwfVJRPzJiaB?= MonzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB{Nj3MOUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTJ3IN88US=> NGrlZpQyOjB{N{ezPS=>
human RS4:11 cells NITteHlEgXSxdH;4bYNqfHliYYPzZZk> NWTjWWhIPzJiaB?= MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSV|Q7OTFiY3XscJMhcGG{Yn;ybY5oKHerbHSgeJlx\SCITGSzJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yO{46KM7:TR?= M17LR|I{PDFzMEez
mouse B16-BL6 cells NYfWXG5QWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVy3NkBp NWPD[IczSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCNVYuSkx4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9N|EvPiEQvF2= MnjSNVIxOjd5M{m=
human H9 cells M3u4fGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFL2XY4{KGSjeYO= NUPhRXBwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUDliY3XscJMh[W[2ZYKgN{Bl[Xm|LDDJR|UxRTN3IN88US=> MliwPFE2QDF4NB?=
human HT1080 cells M{C5XHBzd2yrZnXyZZRqd25iYYPzZZk> M{XRVVczKGh? NGjBVWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUNVA5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSw>? NVy1dI5ZOTJyMke3N|k>
MDCK cells MmD3R5l1d3SxeHnjbZR6KGG|c3H5 NHHQUoVEgXSxdH;4bYNqfHliYXfhbY5{fCCPRFPLJINmdGy|IHL5JG1VXCCjc4PhfUwhS0N3ME2zPU42QSEQvF2= NXjFPXM{OTh4NECwOFI>
mouse L929 cells NEHEPIJHfW6ldHnvckBie3OjeR?= NGLiUWcyPSCvaX7z MXXQc5RmdnSrYYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iVF7GMYFteGijLXnu[JVk\WRiY4n0c5RwgGmlaYT5JI9nKG2xdYPlJGw6OjliY3XscJMh[XO|ZYPz[YQh[XNic4Xyeol3[WyrdImgdJJmcW6ldXLheIVlKG[xcjCxOUBucW6|IHLl[o9z\SCWTl\hcJBp[SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAzPCCqcoOgZpkh[3K7c4ThcEB3cW:uZYSgd5RicW6rbne= NUDxZod5QTJ6N{SxOS=>
human THP1 cells M2PGS2Z2dmO2aX;uJIF{e2G7 M3m1SVIxKHWP NHnObYoyKGh? NHzkWmVKdmirYnn0bY9vKG:oIF7PXFIhcW5iaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDkc5dvemWpdXzheIlwdiCxZjDUVGEucW6mdXPl[EBETDN4IH3SUmEh\XiycnXzd4lwdiCjdDCyNEB2VSCrbnP1ZoF1\WRiZn;yJFEhcHJicILpc5IhfG9iVGDBJINp[WyuZX7n[UBu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgVnQuWEOUIHHuZYx6e2m| MlfVNlM4QDZ3MkC=
MDA-MB-231 cells NWX1Z3hmTnWwY4Tpc44h[XO|YYm= M4fWfVUhfU1? Mmq5TY5pcWKrdHnvckBw\iCSTVGtd5RqdXWuYYTl[EBPTi2tYYDwZWIhe2mpbnHsbY5oKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgOUB2VSCrbnP1ZoF1\WRiZn;yJFE3KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NUSwNms2OjVzOUC0OlY>

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: heterozygous C57BL/TGN TRAMP mice
  • Formulation: 0.5% methyl cellulose and 0.025% Tween 20
  • 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03526081 Active not recruiting Healthy University of California Davis|Mars Inc. January 20 2015 Not Applicable
NCT03526081 Active not recruiting Healthy University of California Davis|Mars Inc. January 20 2015 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID