Apigenin (LY 080400)
For research use only.
Catalog No.S2262 Synonyms: NSC 83244
CAS No. 520-36-5
Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
Selleck's Apigenin (LY 080400) has been cited by 17 publications
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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 (LY 080400) 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 (LY 080400) 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 (LY 080400) purchased from Selleck.
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Choose Selective P450 (e.g. CYP17) Inhibitors
|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.|
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.  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.  Apigenin inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. Apigenin also inhibits proliferating of human keratinocytes. 
|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.  Apigenin (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice. |
-  Lin JK, et al. J Cell Biochem Suppl, 1997, 28-29, 39-48.
-  Shukla S, et al. Pharm Res, 2010, 27(6), 962-978.
-  Balasubramanian S, et al. Toxicol Appl Pharmacol, 2007, 224(3), 214-219.
|In vitro||DMSO||54 mg/mL (199.82 mM)|
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Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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