Apigenin (LY 080400)

Catalog No.S2262 Synonyms: NSC 83244

For research use only.

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

Apigenin (LY 080400) Chemical Structure

CAS No. 520-36-5

Selleck's Apigenin (LY 080400) has been cited by 19 publications

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Other P450 (e.g. CYP17) Products

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 NYnM[WpvTnWwY4Tpc44h[XO|YYm= NVLmc2JsUW6qaXLpeIlwdiCxZjDDU3gzKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{whUUN3ME2wMlUh|ryP MX:xOlA{QDV|Nh?=
human H295R cells MXLGeY5kfGmxbjDhd5NigQ>? Mn;nTY5pcWKrdHnvckBw\iCjcn;tZZRie2ViZYjwdoV{e2WmIHnuJIh2dWGwIFiyPVVTKGOnbHzzMEBKSzVyPUGg{txO NXezO4FmOTh5N{i5OFQ>
HEK293 FS cells M3H0UmZ2dmO2aX;uJIF{e2G7 M134bGlvcGmkaYTpc44hd2ZiTl;YOEBmgHC{ZYPz[YQhcW5iSFXLNlk{KE[VIHPlcIx{KGG|c3Xzd4VlKGG|IFiyU|IheHKxZIXjeIlwdiCkeTDINm8zN1S7cj;MVG8h[XO|YYmsJGlEPTB;MT6xN{DPxE1? MmraNlA4OzF|NUe=
human HeLa cells MoLHSpVv[3Srb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKE2UUEGgeJJidnOoZXP0[YQhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFt|SG3MWGM1KHS{YX7zdI9zfCCkeTDyZZBq\CCoaXz0doF1cW:wIHHzd4F6NCCNaU2yMlQh|ryP M{\PTlE6PzJ3NUe4
human MV4-11 cells M3TsPWN6fG:2b4jpZ4l1gSCjc4PhfS=> MXm3NkBp Mk\CR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGijcnLvdolv\yCITGSzJI12fGG2aX;uJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yMlgyKM7:TR?= NGezXpIzOzRzMUC3Ny=>
human mast cells MojjSpVv[3Srb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKFO\SzDpckBpfW2jbjDtZZN1KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDtZZN1KGOnbHyg[IVoemGwdXzheIlwdixiRVO1NF0{KM7:TR?= M4Hh[FIyOzV2OECw
MDCK cells M{nxd2Z2dmO2aX;uJIF{e2G7 MnzwTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IIXzbY5oKEixZXPod5QhOzN|NEKgd5RicW6rbnesJGlEPTB;Mz6xJO69VQ>? MVmyNVM2PDhyMB?=
human MDA-kb2 cells NYeyUXJvTnWwY4Tpc44h[XO|YYm= NHjsd4dCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIF3ERU1s[jJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFUFRvaX7keYNm\CCudXPp[oVz[XOnIHHjeIl3cXS7IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF02NjJizszN MoHWNVk2QTJ{NEW=
MCF-7 MX cells M3[xcGZ2dmO2aX;uJIF{e2G7 NV3oZppGUW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CCrbjDNR2YuPyCPWDDj[YxteyC3c3nu[{BJd2WlaIP0JFM{OzR{IIP0ZYlvcW6pLDDJR|UxRTVwOTFOwG0> MUOyNVM2PDhyMB?=
mouse RAW264.7 cells MkexSpVv[3Srb36gZZN{[Xl? MYCyOEBp NGmyO2tCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCwaYTybZRmKGGlY4XteYxifGmxbjDh[pRmeiB{NDDodpMh[nliR4Lp[ZN{KHKnYXflcpQhdWW2aH;kMEBKSzVyPU[uO{DPxE1? MYmxPVc4QDB6Nh?=
human H9 cells NGjRfppHfW6ldHnvckBie3OjeR?= NVS0VWkyOyCmYYnz MYjBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIFi5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhOyCmYYnzJIJ6KHB{NDDhcpRq\2WwIHPhdJR2emViYYPzZZktKEWFNUC9PUDPxE1? NVPLW3VCQDF3OEG2OC=>
HEK293 cells NHrjVGVHfW6ldHnvckBie3OjeR?= M1\I[FI1KGh? M3GyV2Fod26rc4SgZYN1cX[rdImgZZQhdW:3c3WgVHBCWmejbX3hJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ48u\XiycnXzd4lv\yC5aYToJGdidDRicnXwc5J1\XJidnXjeI9zKGGodHXyJFI1KGi{czDifUBlfWGuLXz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFXDOVA:OjRwOTFOwG0> M4HBNFI1QTV3OEi5
mouse 26-L5 cells NGHBZXdRem:uaX\ldoF1cW:wIHHzd4F6 MlvrO|IhcA>? MkX2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB{Nj3MOUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTJ3IN88US=> MXKxNlAzPzd|OR?=
human RS4:11 cells NVP0PYJ{S3m2b4TvfIlkcXS7IHHzd4F6 MX[3NkBp Moj5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnM1QjFzIHPlcIx{KGijcnLvdolv\yC5aXzkJJR6eGViRlzUN{Bi\nSncjC3NkBpenNiYomgeIV1emG8b3zpeY0h[mG|ZXSgSZohS3mWb4igZ4VtdCC4aXHibYxqfHliYYPzZZktKEeLNUC9NlcvQSEQvF2= MYKyN|QyOTB5Mx?=
mouse B16-BL6 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MmK1O|IhcA>? NXjteHpXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCNVYuSkx4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9N|EvPiEQvF2= NX[2ZoxUOTJyMke3N|k>
human H9 cells MnLqR5l1d3SxeHnjbZR6KGG|c3H5 MnP1N{Bl[Xm| NHjUeHVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJQSClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OzVizszN MX24NVU5OTZ2
human HT1080 cells NUTmS2tMWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1e1O|czKGh? MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWMUC4NEBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJRy=> NECxbVIyOjB{N{ezPS=>
MDCK cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= NF;0W|NEgXSxdH;4bYNqfHliYXfhbY5{fCCPRFPLJINmdGy|IHL5JG1VXCCjc4PhfUwhS0N3ME2zPU42QSEQvF2= NWPHN3l6OTh4NECwOFI>
mouse L929 cells NEPQbFBHfW6ldHnvckBie3OjeR?= M{DkcVE2KG2rboO= MnnpVI91\W62aXH0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIGTOSk1idHCqYT3pcoR2[2WmIHP5eI91d3irY3n0fUBw\iCvb4Xz[UBNQTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dpZqfmGuaYT5JJBz\WmwY4XiZZRm\CCob4KgNVUhdWmwczDi[YZwemViVF7GZYxxcGFiYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOjRiaILzJIJ6KGO{eYP0ZYwhfmmxbHX0JJN1[WmwaX7n M3HRR|kzQDd2MUW=
human THP1 cells M1LURWZ2dmO2aX;uJIF{e2G7 MVOyNEB2VQ>? MonCNUBp MmS1TY5pcWKrdHnvckBw\iCQT2iyJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZiVGDBMYlv\HWlZXSgR2Q{PiCvUl7BJIV5eHKnc4Ppc44h[XRiMkCgeW0hcW6ldXLheIVlKG[xcjCxJIhzKHC{aX;yJJRwKFSSQTDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? NIHlRnMzOzd6NkWyNC=>
MDA-MB-231 cells M{fwPGZ2dmO2aX;uJIF{e2G7 MlPsOUB2VQ>? NUnudFZoUW6qaXLpeIlwdiCxZjDQUWEue3SrbYXsZZRm\CCQRj3rZZBx[UJic3nncoFtcW6pIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPSC3TTDpcoN2[mG2ZXSg[o9zKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NY[5UZJ6OjVzOUC0OlY>
Assay
Methods Test Index PMID
Western blot MHC / MHC2A / MHC2B / MyoD ; CXCR4 ; CDK1 / Cyclin B1 / p21 29108230 23743303 24009741
Immunofluorescence E-caherin / Vimentin ; Snail 27203387
Growth inhibition assay Cell viability 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 (from reference)

Cell Research:

[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.

  • (Only for Reference)
Animal Research:

[6]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
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