kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
Apigenin, 100 mg  

Apigenin, 100 mg

Apigenin is a MAP kinase (MAPK/ERK) inhibitor, 4',5,7-Trihydroxyflavone

antioxidant flavonoid showing activity against MAP kinase (MAPK/ERK), ERK inhibitor, CAS number: 520-36-5

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80,00 €

Background: Apigenin is an antioxidant flavonoid showing cell type specific effects on a number of MAPK. Thus, apigenin was found to sustain the activation of ERK1/2 phosphorylation induced by EGF stimulation in PC12 cells whereas whereas an inhibition of ERK1/2 activation was reported in rapidly proliferating cells and in thyroid cancer cells. Apigenin inhibits the proliferation of malignant tumor cells by G2/M arrest and induces apoptosis with high efficacy in myelogenous leukemia cells. Apigenin induces phosphorylation of Hsp27, leading to a decreased Hsp27 chaperone activity which confers cells resistance to chemotherapeutic drugs.

Appearance: Light yellow powder
Purity: 90%
Solubility: Soluble in diluted potassium hydroxide or DMSO, slightly soluble in 100% ethanol (hot), insoluble in water
Hazard: Irritant
Molecular weight: 270.2 g/mol
Formula: C15H10O5
CAS number: 520-36-5

Product specific literature references:

Sato F, Matsukawa Y, Sakai T et al. (1994) "Apigenin induces morphological differentiation and G2-M arrest in rat neuronal cells" Biochem Biophys Res Commun. 204(2):578-84

Kuo ML, Yang NC (1995) "Reversion of v-H-ras-transformed NIH 3T3 cells by apigenin through inhibiting mitogen activated protein kinase and its downstream oncogenes" Biochem Biophys Res Commun. 212(3):767-75

Lepley DM, Li B, Birt DF, Pelling JC (1996) "The chemopreventive flavonoid apigenin induces G2/M arrest in keratinocytes" Carcinogenesis 17(11):2367-75

Birt DF, Mitchell D, Gold B, Pour P, Pinch HC (1997) "Inhibition of ultraviolet light induced skin carcinogenesis in SKH-1 mice by apigenin, a plant flavonoid" Anticancer Res. 17(1A):85-91

Lepley DM, Pelling JC (1997) "Induction of p21/WAF1 and G1 cell-cycle arrest by the chemopreventive agent apigenin" Mol Carcinog. 19(2):74-82.

Wang IK, Lin-Shiau SY, Lin JK (1999) "Induction of apoptosis by apigenin and related flavonoids through cytochrome c release and activation of caspase-9 and caspase-3 in leukaemia HL-60 cells" Eur J Cancer 35(10):1517-25

Yin F, Giuliano AE, Van Herle AJ (1999) "Signal pathways involved in apigenin inhibition of growth and induction of apoptosis of human anaplastic thyroid cancer cells (ARO)" Anticancer Res. 19(5B):4297-303

Trochon V, Blot E, Soria C et al. (2000) "Apigenin inhibits endothelial-cell proliferation in G(2)/M phase whereas it stimulates smooth-muscle cells by inhibiting P21 and P27 expression" Int J Cancer 85(5):691-6

Caltagirone S, Rossi C, Piantelli M et al. (2000) "Flavonoids apigenin and quercetin inhibit melanoma growth and metastatic potential" Int J Cancer 87(4):595-600

Gupta S, Afaq F, Mukhtar H (2001) "Selective growth-inhibitory, cell-cycle deregulatory and apoptotic response of apigenin in normal versus human prostate carcinoma cells" Biochem Biophys Res Commun. 287(4):914-20

Yin F, Giuliano AE, Law RE, Van Herle AJ (2001) "Apigenin inhibits growth and induces G2/M arrest by modulating cyclin-CDK regulators and ERK MAP kinase activation in breast carcinoma cells" Anticancer Res. 21(1A):413-20

Lindenmeyer F, Li H, Menashi S, Soria C, Lu​‌ H (2001) "Apigenin Acts on the Tumor Cell Invasion Process and Regulates Protease Production" Nutrition and Cancer 39, 1, 139-147

Llorens F, Garcia L, Itarte E, Gomez N (2002) "Apigenin and LY294002 prolong EGF-stimulated ERK1/2 activation in PC12 cells but are unable to induce full differentiation" FEBS Lett. 510(3):149-53

Way TD, Kao MC, Lin JK (2004) "Apigenin induces apoptosis through proteasomal degradation of HER2/neu in HER2/neu-overexpressing breast cancer cells via the phosphatidylinositol 3-kinase/Akt-dependent pathway" J Biol Chem. 279(6):4479-89

Van Dross R, Xue Y, Knudson A, Pelling JC. (2003) “The chemopreventive bioflavonoid apigenin modulates signal transduction pathways in keratinocyte and colon carcinoma cell lines.” J Nutr. 133(11 Suppl 1):3800S-3804S.

M E Gonzalez-Mejia, O H Voss, E J Murnan and A I Doseff (2010)  “Apigenin-induced apoptosis of leukemia cells is mediated by a bimodal and differentially regulated residue-specific phosphorylation of heat-shock protein–27” Cell Death Dis. 19;1(8):e64.

Product Citations:

Boeckx C, Op de Beeck K, Wouters A, Deschoolmeester V, Limame R, Zwaenepoel K, Specenier P, Pauwels P, Vermorken JB, Peeters M, Van Camp G, Baay M, Lardon F. (2014) "Overcoming cetuximab resistance in HNSCC: the role of AURKB and DUSP proteins."Cancer Lett. 2014 Nov 28;354(2):365-77.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.   

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