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 5 Publications

4 Customer Reviews

  • 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.

    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.

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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 MX3GeY5kfGmxbjDhd5NigQ>? NFnDeI5KdmirYnn0bY9vKG:oIFPPXFIheHKxdHXpckBmgHC{ZYPzbY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzMEBKSzVyPUCuOUDPxE1? MVGxOlA{QDV|Nh?=
human H295R cells MYjGeY5kfGmxbjDhd5NigQ>? NHzGS2pKdmirYnn0bY9vKG:oIHHyc41ifGG|ZTDlfJBz\XO|ZXSgbY4hcHWvYX6gTFI6PVJiY3XscJMtKEmFNUC9NUDPxE1? MVOxPFc4QDl2NB?=
HEK293 FS cells MX;GeY5kfGmxbjDhd5NigQ>? M{SxfmlvcGmkaYTpc44hd2ZiTl;YOEBmgHC{ZYPz[YQhcW5iSFXLNlk{KE[VIHPlcIx{KGG|c3Xzd4VlKGG|IFiyU|IheHKxZIXjeIlwdiCkeTDINm8zN1S7cj;MVG8h[XO|YYmsJGlEPTB;MT6xN{DPxE1? M4Dyd|IxPzNzM{W3
human HeLa cells MX3GeY5kfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKE2UUEGgeJJidnOoZXP0[YQhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFt|SG3MWGM1KHS{YX7zdI9zfCCkeTDyZZBq\CCoaXz0doF1cW:wIHHzd4F6NCCNaU2yMlQh|ryP NFv6PZgyQTd{NUW3PC=>
human MV4-11 cells MVLDfZRwfG:6aXPpeJkh[XO|YYm= NUSzTXJQPzJiaB?= M3TkcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1XPC1zMTDj[YxteyCqYYLic5JqdmdiRlzUN{BufXSjdHnvckBi\nSncjC3NkBpenNiYomgeIV1emG8b3zpeY0h[mG|ZXSgSZohS3mWb4igZ4VtdCC4aXHibYxqfHliYYPzZZktKEeLNUC9Nk45OSEQvF2= NG\nbZkzOzRzMUC3Ny=>
human mast cells NXzQZlM3TnWwY4Tpc44h[XO|YYm= M2\1PGlvcGmkaYTpc44hd2ZiU2nLJIlvKGi3bXHuJI1ie3RiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJI1ie3RiY3XscEBl\We{YX71cIF1cW:wLDDFR|UxRTNizszN NVvjZnJ3OjF|NUS4NFA>
MDCK cells MWPGeY5kfGmxbjDhd5NigQ>? M4PI[mlvcGmkaYTpc44hd2ZiQlPSVEBmgHC{ZYPz[YQhcW5iTVTDT{Bk\WyuczD1d4lv\yCKb3XjbJN1KDN|M{SyJJN1[WmwaX7nMEBKSzVyPUOuNUDPxE1? NF;aRmYzOTN3NEiwNC=>
human MDA-kb2 cells MYrGeY5kfGmxbjDhd5NigQ>? NUP3fZlVSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDpckBpfW2jbjDNSGEuc2J{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRibIXjbYZmemG|ZTDhZ5Rqfmm2eTDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:PS5{IN88US=> NGnq[FUyQTV7MkK0OS=>
MCF-7 MX cells M1HJcGZ2dmO2aX;uJIF{e2G7 MlvsTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EBqdiCPQ1[tO{BOYCClZXzsd{B2e2mwZzDIc4VkcHO2IEOzN|QzKHO2YXnubY5oNCCLQ{WwQVUvQSEQvF2= MXGyNVM2PDhyMB?=
mouse RAW264.7 cells NHTRfZlHfW6ldHnvckBie3OjeR?= NEDtR2wzPCCq MXPBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHnZYlve3RibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBvcXS{aYTlJIFk[3WvdXzheIlwdiCjZoTldkAzPCCqcoOgZpkhT3KrZYPzJJJm[WenboSgcYV1cG:mLDDJR|UxRTZwNzFOwG0> MUOxPVc4QDB6Nh?=
human H9 cells MnW5SpVv[3Srb36gZZN{[Xl? MmT2N{Bl[Xm| M4Dvd2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gTFkh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDh[pRmeiB|IHThfZMh[nlicEK0JIFvfGmpZX6gZ4FxfHW{ZTDhd5NigSxiRVO1NF06KM7:TR?= NVjKOohLQDF3OEG2OC=>
HEK293 cells NYXm[od5TnWwY4Tpc44h[XO|YYm= NH7Td3kzPCCq MWTB[49vcXO2IHHjeIl3cXS7IHH0JI1wfXOnIGDQRXJo[W2vYTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHPvMYV5eHKnc4Ppcochf2m2aDDHZYw1KHKncH;yeIVzKH[nY4TvdkBi\nSncjCyOEBpenNiYomg[JVidC2udXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCHQ{WwQVI1NjlizszN MWqyOFk2PTh6OR?=
mouse 26-L5 cells M4\sbXBzd2yrZnXyZZRqd25iYYPzZZk> NXjmUGY6PzJiaB?= NVSwXmZ{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTCyOk1NPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUK1JO69VQ>? NVftRnFrOTJyMke3N|k>
human RS4:11 cells M{jmRmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWC4dVVSPzJiaB?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSV|Q7OTFiY3XscJMhcGG{Yn;ybY5oKHerbHSgeJlx\SCITGSzJIFnfGW{IEeyJIhzeyCkeTD0[ZRz[XqxbHn1cUBj[XOnZDDFfkBEgVSxeDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhT0l3ME2yO{46KM7:TR?= NVTrNJI5OjN2MUGwO|M>
mouse B16-BL6 cells NVOzdJQ4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MmTxO|IhcA>? NETx[4ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFKxOk1DVDZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhTUN3ME2zNU43KM7:TR?= MnjhNVIxOjd5M{m=
human H9 cells NE[4NWFEgXSxdH;4bYNqfHliYYPzZZk> M16xN|Mh\GG7cx?= MnH1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFkh[2WubIOgZYZ1\XJiMzDkZZl{NCCLQ{WwQVM2KM7:TR?= MWS4NVU5OTZ2
human HT1080 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 MYe3NkBp M3uw[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSxNFgxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlE NGTmPXUyOjB{N{ezPS=>
MDCK cells NXfKdHE2S3m2b4TvfIlkcXS7IHHzd4F6 NUG5OHM4S3m2b4TvfIlkcXS7IHHnZYlve3RiTVTDT{Bk\WyuczDifUBOXFRiYYPzZZktKEOFNUC9N|kvPTlizszN NXzidVB2OTh4NECwOFI>
mouse L929 cells NYS4NIZ4TnWwY4Tpc44h[XO|YYm= NXuxXmNlOTVibXnudy=> MmjYVI91\W62aXH0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIGTOSk1idHCqYT3pcoR2[2WmIHP5eI91d3irY3n0fUBw\iCvb4Xz[UBNQTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dpZqfmGuaYT5JJBz\WmwY4XiZZRm\CCob4KgNVUhdWmwczDi[YZwemViVF7GZYxxcGFiYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOjRiaILzJIJ6KGO{eYP0ZYwhfmmxbHX0JJN1[WmwaX7n MV:5Nlg4PDF3
human THP1 cells M4H5WWZ2dmO2aX;uJIF{e2G7 MoDiNlAhfU1? MlH5NUBp Ml:zTY5pcWKrdHnvckBw\iCQT2iyJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZiVGDBMYlv\HWlZXSgR2Q{PiCvUl7BJIV5eHKnc4Ppc44h[XRiMkCgeW0hcW6ldXLheIVlKG[xcjCxJIhzKHC{aX;yJJRwKFSSQTDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? NVPFbWhsOjN5OE[1NlA>
MDA-MB-231 cells MV7GeY5kfGmxbjDhd5NigQ>? MmPWOUB2VQ>? NWPsRXNNUW6qaXLpeIlwdiCxZjDQUWEue3SrbYXsZZRm\CCQRj3rZZBx[UJic3nncoFtcW6pIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPSC3TTDpcoN2[mG2ZXSg[o9zKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NHmx[lYzPTF7MES2Oi=>

... 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