Apigenin (LY 080400)

For research use only.

Catalog No.S2262 Synonyms: NSC 83244

17 publications

Apigenin (LY 080400) Chemical Structure

CAS No. 520-36-5

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

Selleck's Apigenin (LY 080400) has been cited by 17 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 (LY 080400) 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 (LY 080400) 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 (LY 080400) 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 (LY 080400) purchased from Selleck.

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

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 NH3t[3VHfW6ldHnvckBie3OjeR?= Ml3GTY5pcWKrdHnvckBw\iCFT2iyJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczygTWM2OD1yLkWg{txO MlrONVYxOzh3M{[=
human H295R cells MVHGeY5kfGmxbjDhd5NigQ>? M1rFbmlvcGmkaYTpc44hd2ZiYYLvcYF1[XOnIHX4dJJme3OnZDDpckBpfW2jbjDINlk2WiClZXzsd{whUUN3ME2xJO69VQ>? NHv1PG8yQDd5OEm0OC=>
HEK293 FS cells MYjGeY5kfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKE6RWESg[ZhxemW|c3XkJIlvKEiHS{K5N{BHWyClZXzsd{Bie3Onc4Pl[EBieyCKMl:yJJBzd2S3Y4Tpc44h[nliSELPNk9VgXJxTGDPJIF{e2G7LDDJR|UxRTFwMUOg{txO NHrxUlYzODd|MUO1Oy=>
human HeLa cells NWLJXFhSTnWwY4Tpc44h[XO|YYm= NXzEelBoUW6qaXLpeIlwdiCxZjDNVnAyKHS{YX7z[oVkfGWmIHnuJIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbN2heVFSFNDD0doFve3CxcoSgZpkhemGyaXSg[oltfHKjdHnvckBie3OjeTygT4k:Oi52IN88US=> NF3LfGIyQTd{NUW3PC=>
human MV4-11 cells MkDtR5l1d3SxeHnjbZR6KGG|c3H5 NF\ofpc4OiCq MoD6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGijcnLvdolv\yCITGSzJI12fGG2aX;uJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yMlgyKM7:TR?= NIDNZ5kzOzRzMUC3Ny=>
human mast cells NGnifVZHfW6ldHnvckBie3OjeR?= M372dGlvcGmkaYTpc44hd2ZiU2nLJIlvKGi3bXHuJI1ie3RiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJI1ie3RiY3XscEBl\We{YX71cIF1cW:wLDDFR|UxRTNizszN MnHUNlE{PTR6MEC=
MDCK cells M33LT2Z2dmO2aX;uJIF{e2G7 MXTJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2GQ1ugZ4VtdHNidYPpcochUG:nY3jzeEA{OzN2MjDzeIFqdmmwZzygTWM2OD1|LkGg{txO MVWyNVM2PDhyMB?=
human MDA-kb2 cells NFTwbVZHfW6ldHnvckBie3OjeR?= NGXVVWZCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIF3ERU1s[jJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFUFRvaX7keYNm\CCudXPp[oVz[XOnIHHjeIl3cXS7IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF02NjJizszN MmjBNVk2QTJ{NEW=
MCF-7 MX cells MY\GeY5kfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2FRj23JG1ZKGOnbHzzJJV{cW6pIFjv[YNpe3RiM{OzOFIhe3SjaX7pcoctKEmFNUC9OU46KM7:TR?= NY\aWnBQOjF|NUS4NFA>
mouse RAW264.7 cells MYXGeY5kfGmxbjDhd5NigQ>? MlPMNlQhcA>? M17GN2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKG6rdILpeIUh[WOldX31cIF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCJcnnld5MhemWjZ3XueEBu\XSqb3SsJGlEPTB;Nj63JO69VQ>? NV74TJk4OTl5N{iwPFY>
human H9 cells NF63cVJHfW6ldHnvckBie3OjeR?= NFXicnQ{KGSjeYO= NHWxXJFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIlv\mWldHXkJIlvKGi3bXHuJGg6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxicnXwcIlk[XSrb36gZYZ1\XJiMzDkZZl{KGK7IICyOEBidnSrZ3XuJINieHS3cnWgZZN{[XluIFXDOVA:QSEQvF2= M3jYTFgyPThzNkS=
HEK293 cells MVLGeY5kfGmxbjDhd5NigQ>? M3OxS|I1KGh? MmjyRYdwdmm|dDDhZ5Rqfmm2eTDheEBud3W|ZTDQVGFT\2GvbXGg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{1mgHC{ZYPzbY5oKHerdHigS4FtPCC{ZYDvdpRmeiC4ZXP0c5Ih[W[2ZYKgNlQhcHK|IHL5JIR2[WxvbIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiRVO1NF0zPC57IN88US=> MYWyOFk2PTh6OR?=
mouse 26-L5 cells Moq0VJJwdGmoZYLheIlwdiCjc4PhfS=> MnjNO|IhcA>? MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKDJ4LVy1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFXDOVA:OjVizszN M175blEzODJ5N{O5
human RS4:11 cells MlrvR5l1d3SxeHnjbZR6KGG|c3H5 MmP4O|IhcA>? MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSV|Q7OTFiY3XscJMhcGG{Yn;ybY5oKHerbHSgeJlx\SCITGSzJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yO{46KM7:TR?= NYXs[G5POjN2MUGwO|M>
mouse B16-BL6 cells MlLUVJJwdGmoZYLheIlwdiCjc4PhfS=> NU\ZWWVIPzJiaB?= NYOySHMzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCNVYuSkx4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9N|EvPiEQvF2= MmXyNVIxOjd5M{m=
human H9 cells M17RR2N6fG:2b4jpZ4l1gSCjc4PhfS=> MUKzJIRigXN? MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIPUBk\WyuczDh[pRmeiB|IHThfZMtKEmFNUC9N|Uh|ryP MV24NVU5OTZ2
human HT1080 cells MkHFVJJwdGmoZYLheIlwdiCjc4PhfS=> NXnnXGZnPzJiaB?= MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWMUC4NEBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJRy=> MXexNlAzPzd|OR?=
MDCK cells NHnRWZVEgXSxdH;4bYNqfHliYYPzZZk> MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{KGK7IF3UWEBie3OjeTygR2M2OD1|OT61PUDPxE1? NVu3W2NDOTh4NECwOFI>
mouse L929 cells NYLYXo5jTnWwY4Tpc44h[XO|YYm= NHTmSIsyPSCvaX7z M3jGcnBwfGWwdHnheIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDUUmYu[WyyaHGtbY5lfWOnZDDjfZRwfG:6aXPpeJkhd2ZibX;1d4UhVDl{OTDj[YxteyCjc4Pld5Nm\CCjczDzeZJ3cX[jbHn0fUBxemWrbnP1ZoF1\WRiZn;yJFE2KG2rboOgZoVnd3KnIGTOSoFteGijIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSClconzeIFtKH[rb3zleEB{fGGrbnnu[y=> M{DU[FkzQDd2MUW=
human THP1 cells NELYbWVHfW6ldHnvckBie3OjeR?= NFz3NFAzOCC3TR?= MWKxJIg> NXfYcoJWUW6qaXLpeIlwdiCxZjDOU3gzKGmwIHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gWHBCNWmwZIXj[YQhS0R|NjDtVm5CKGW6cILld5Nqd25iYYSgNlAhfU1iaX7jeYJifGWmIH\vdkAyKGi{IIDybY9zKHSxIGTQRUBkcGGubHXu[4UhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= NXjNO2pTOjN5OE[1NlA>
MDA-MB-231 cells MkXJSpVv[3Srb36gZZN{[Xl? MYK1JJVO M4ny[2lvcGmkaYTpc44hd2ZiUF3BMZN1cW23bHH0[YQhVkZva3HwdIFDKHOrZ37hcIlv\yBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDNSGEuVUJvMkOxJINmdGy|IHH0JFUhfU1iaX7jeYJifGWmIH\vdkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 MmLxNlUyQTB2Nk[=

... 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]

- Collapse
  • 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]

- Collapse
  • 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
Smiles C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

P450 (e.g. CYP17) Signaling Pathway Map

P450 (e.g. CYP17) Inhibitors with Unique Features

Related P450 (e.g. CYP17) Products

Tags: buy Apigenin (LY 080400) | Apigenin (LY 080400) supplier | purchase Apigenin (LY 080400) | Apigenin (LY 080400) cost | Apigenin (LY 080400) manufacturer | order Apigenin (LY 080400) | Apigenin (LY 080400) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID