Apigenin

BML-EI345

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Antioxidant and chemopreventive

Apigenin is an antioxidant flavonoid. Has chemopreventive and antitumor properties. Induces apoptosis. Inhibits the proliferation of malignant tumor cells by G2/M arrest. Is a MAP-Kinase (MAPK/ERK) inhibitor. Inhibits hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) expression. Induces gastric relaxation in mouse stomach, mainly by suppressing Ca²⁺ influx through voltage-dependent calcium channels. Apigenin is a selective inhibitor of CK2. In WEHI 231 cells inhibition of CK2 by apigenin decreased the rate of IκBα turnover and nuclear levels of NF-κB (20 µM). It blocks proliferation of Wnt-1 transfected cells and abrogates phosphorylation of β-catenin. In a rat model of glomerulonephritis, inhibition of CK2 by apigenin ameliorates renal dysfunction.

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Product Details

Appearance	light yellow to slightly brown powder
CAS	520-36-5
Couple Target	Casein kinase, HIF, MAPK
Couple Type	Inhibitor
Formula	C₁₅H₁₀O₅
MW	270.2
Purity	≥97% (HPLC)
Solubility	Soluble in diluted potassium hydroxyde or DMSO, slightly soluble in 100% ethanol (hot). Insoluble in water.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Flavonoids from Ericameria nauseosa inhibiting PI3K/AKT pathway in human melanoma cells: T. Hell, et al.; Biomed. Pharmacother. 156, 113754 (2022), Abstract
Enzymatic synthesis of α-flavone glucoside via regioselective transglucosylation by amylosucrase from Deinococcus geothermalis: S.W. Jang, et al.; PLoS One 13, e0207466 (2018), Abstract
Gastric relaxation induced by apigenin and quercetin: analysis of the mechanism of action: A. Rotondo et al.; Life. Sci. 85, 85 (2009), Abstract
Apigenin blocks lipopolysaccharide-induced lethality in vivo and proinflammatory cytokines expression by inactivating NF-kappaB through the suppression of p65 phosphorylation: C. Nicholas et al.; J. Immunol. 179, 7121 (2007), Abstract
Apigenin-induced cell cycle arrest is mediated by modulation of MAPK, PI3K-Akt, and loss of cyclin D1 associated retinoblastoma dephosphorylation in human prostate cancer cells: S. Shukla & S. Gupta; Cell Cycle 6, 1102 (2007), Abstract
Apigenin inhibits tumor angiogenesis through decreasing HIF-1alpha and VEGF expression: J. Fang et al.; Carcinogenesis 28, 858 (2007), Abstract
Apigenin and cancer chemoprevention: progress, potential and promise (review): D. Patel et al.; Int. J. Oncol. 30, 233 (2007), Abstract
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=10699950: R. Torkin et al.; Mol. Cancer. Ther. 4, 1 (2005), Abstract
Inhibition of protein kinase CK2 prevents the progression of glomerulonephritis: M. Yamada et al.; PNAS 102, 7736 (2005), Abstract
Phosphorylation by the protein kinase CK2 promotes calpain-mediated degradation of IkappaBalpha: J. Shen et al.; J. Immunol. 167, 4919 (2001), Abstract

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Apigenin

BML-EI345

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