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 22 publications

Purity & Quality Control

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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 NVLjWJhPTnWwY4Tpc44h[XO|YYm= M32yeGlvcGmkaYTpc44hd2ZiQ1;YNkBxem:2ZXnuJIV5eHKnc4Ppc44hcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOsJGlEPTB;MD61JO69VQ>? NWX2W21ZOTZyM{i1N|Y>
human H295R cells M2ex[mZ2dmO2aX;uJIF{e2G7 NVXQcIhEUW6qaXLpeIlwdiCxZjDhdo9u[XSjc3Wg[ZhxemW|c3XkJIlvKGi3bXHuJGgzQTWUIHPlcIx{NCCLQ{WwQVEh|ryP NYTIeWNlOTh5N{i5OFQ>
HEK293 FS cells MnXxSpVv[3Srb36gZZN{[Xl? NIS3PJhKdmirYnn0bY9vKG:oIF7PXFQh\XiycnXzd4VlKGmwIFjFT|I6OyCIUzDj[YxteyCjc4Pld5Nm\CCjczDINm8zKHC{b3T1Z5Rqd25iYomgTFJQOi:WeYKvUHBQKGG|c3H5MEBKSzVyPUGuNVMh|ryP M3XWW|IxPzNzM{W3
human HeLa cells MkP2SpVv[3Srb36gZZN{[Xl? Mor4TY5pcWKrdHnvckBw\iCPUmCxJJRz[W6|ZnXjeIVlKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdM1jdUHREPCC2cnHud5BwenRiYomgdoFxcWRiZnnseJJifGmxbjDhd5NigSxiS3m9Nk41KM7:TR?= NWi2eY12OTl5MkW1O|g>
human MV4-11 cells NXH3NWI6S3m2b4TvfIlkcXS7IHHzd4F6 NIDUVoU4OiCq MoXZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGijcnLvdolv\yCITGSzJI12fGG2aX;uJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yMlgyKM7:TR?= M{DKSFI{PDFzMEez
human mast cells MVLGeY5kfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKFO\SzDpckBpfW2jbjDtZZN1KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDtZZN1KGOnbHyg[IVoemGwdXzheIlwdixiRVO1NF0{KM7:TR?= MnPoNlE{PTR6MEC=
MDCK cells M1fYSWZ2dmO2aX;uJIF{e2G7 MkTKTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IIXzbY5oKEixZXPod5QhOzN|NEKgd5RicW6rbnesJGlEPTB;Mz6xJO69VQ>? M1nYdVIyOzV2OECw
human MDA-kb2 cells NEDxcWFHfW6ldHnvckBie3OjeR?= NXLOemk2SW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDpckBpfW2jbjDNSGEuc2J{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRibIXjbYZmemG|ZTDhZ5Rqfmm2eTDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:PS5{IN88US=> NWPse4F3OTl3OUKyOFU>
MCF-7 MX cells MmO5SpVv[3Srb36gZZN{[Xl? NHfRZ2pKdmirYnn0bY9vKG:oIFLDVnAh\XiycnXzd4VlKGmwIF3DSk04KE2[IHPlcIx{KHW|aX7nJGhw\WOqc4SgN|M{PDJic4ThbY5qdmduIFnDOVA:PS57IN88US=> M1zhN|IyOzV2OECw
mouse RAW264.7 cells MVTGeY5kfGmxbjDhd5NigQ>? MV:yOEBp M{KxfWFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKG6rdILpeIUh[WOldX31cIF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCJcnnld5MhemWjZ3XueEBu\XSqb3SsJGlEPTB;Nj63JO69VQ>? MXixPVc4QDB6Nh?=
human H9 cells MoTBSpVv[3Srb36gZZN{[Xl? MojXN{Bl[Xm| M2qzTWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gTFkh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDh[pRmeiB|IHThfZMh[nlicEK0JIFvfGmpZX6gZ4FxfHW{ZTDhd5NigSxiRVO1NF06KM7:TR?= NFHIWY05OTV6MU[0
HEK293 cells NGfWWlFHfW6ldHnvckBie3OjeR?= MViyOEBp NXHvdo4{SWexbnnzeEBi[3Srdnn0fUBifCCvb4Xz[UBRWEGUZ3HtcYEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bkdy2neIDy[ZN{cW6pIIfpeIghT2GuNDDy[ZBwenSncjD2[YN1d3JiYX\0[ZIhOjRiaILzJIJ6KGS3YXytcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygSWM2OD1{ND65JO69VQ>? NUTKcJIyOjR7NUW4PFk>
mouse 26-L5 cells M4HsOXBzd2yrZnXyZZRqd25iYYPzZZk> MV23NkBp Ml7sRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB{Nj3MOUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTJ3IN88US=> MYixNlAzPzd|OR?=
human RS4:11 cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= M37NTlczKGh? M2rUWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJUPDpzMTDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIF\MWFMh[W[2ZYKgO|IhcHK|IHL5JJRmfHKjen;sbZVuKGKjc3XkJGV7KEO7VH;4JINmdGxidnnhZoltcXS7IHHzd4F6NCCJSUWwQVI4NjlizszN NF;HbnYzOzRzMUC3Ny=>
mouse B16-BL6 cells NIGxPXlRem:uaX\ldoF1cW:wIHHzd4F6 Mn:yO|IhcA>? M2P6cWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQkG2MWJNPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUOxMlYh|ryP NYrLdmJ2OTJyMke3N|k>
human H9 cells MkTMR5l1d3SxeHnjbZR6KGG|c3H5 MknTN{Bl[Xm| NIT1SlREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJQSClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OzVizszN MkmzPFE2QDF4NB?=
human HT1080 cells MoPOVJJwdGmoZYLheIlwdiCjc4PhfS=> MY[3NkBp M2LQV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSxNFgxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlE MlvnNVIxOjd5M{m=
MDCK cells MlXmR5l1d3SxeHnjbZR6KGG|c3H5 NHHjR2FEgXSxdH;4bYNqfHliYXfhbY5{fCCPRFPLJINmdGy|IHL5JG1VXCCjc4PhfUwhS0N3ME2zPU42QSEQvF2= MXSxPFY1ODB2Mh?=
mouse L929 cells M2PxbWZ2dmO2aX;uJIF{e2G7 MWSxOUBucW6| MUDQc5RmdnSrYYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iVF7GMYFteGijLXnu[JVk\WRiY4n0c5RwgGmlaYT5JI9nKG2xdYPlJGw6OjliY3XscJMh[XO|ZYPz[YQh[XNic4Xyeol3[WyrdImgdJJmcW6ldXLheIVlKG[xcjCxOUBucW6|IHLl[o9z\SCWTl\hcJBp[SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAzPCCqcoOgZpkh[3K7c4ThcEB3cW:uZYSgd5RicW6rbne= NUGyVFZ6QTJ6N{SxOS=>
human THP1 cells M{fteWZ2dmO2aX;uJIF{e2G7 NUnQZ2p4OjBidV2= MVWxJIg> MYTJcohq[mm2aX;uJI9nKE6RWEKgbY4hcHWvYX6gWGhROSClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCWUFGtbY5lfWOnZDDDSFM3KG2UTlGg[ZhxemW|c3nvckBifCB{MDD1UUBqdmO3YnH0[YQh\m:{IEGgbJIheHKrb4KgeI8hXFCDIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB{NDDodpMh[nliUmStVGNTKGGwYXz5d4l{ MUmyN|c5PjV{MB?=
MDA-MB-231 cells NF:0XphHfW6ldHnvckBie3OjeR?= MnHqOUB2VQ>? NFjQXXlKdmirYnn0bY9vKG:oIGDNRU1{fGmvdXzheIVlKE6ILXvhdJBiSiC|aXfuZYxqdmdiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gUWRCNU2ELUKzNUBk\WyuczDheEA2KHWPIHnuZ5Vj[XSnZDDmc5IhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MlTiNlUyQTB2Nk[=
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.

Animal Research:

[6]

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

Solubility (25°C)

In vitro

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

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