Apigenin

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Apigenin is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well) Natural Product Library (96-well)

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1250	MDV3100 (Enzalutamide)	<1 mg/mL	93 mg/mL	3 mg/mL
S2246	Abiraterone Acetate (CB7630)	<1 mg/mL	<1 mg/mL	28 mg/mL
S1190	Bicalutamide (Casodex)	<1 mg/mL	86 mg/mL	7 mg/mL
S1123	Abiraterone (CB-7598)	<1 mg/mL	0.33 mg/mL	<1 mg/mL
S2187	Avasimibe(CI-1011)	<1 mg/mL	100 mg/mL	8 mg/mL
S1442	Voriconazole	<1 mg/mL	70 mg/mL	20 mg/mL
S1353	Ketoconazole	<1 mg/mL	16 mg/mL	10 mg/mL
S1908	Flutamide (Eulexin)	<1 mg/mL	55 mg/mL	55 mg/mL
S2555	Clarithromycin (Biaxin, Klacid)	<1 mg/mL	18 mg/mL	<1 mg/mL
S2042	Cyproterone acetate	<1 mg/mL	≥83 mg/mL	≥10 mg/mL
S2803	Galeterone (TOK-001)	<1 mg/mL	24 mg/mL	40 mg/mL
S1195	TAK-700 (Orteronel)	<1 mg/mL	62 mg/mL	8 mg/mL
S2526	Alizarin	<1 mg/mL	48 mg/mL	<1 mg/mL
S2046	Pioglitazone HCl (Actos)	<1 mg/mL	79 mg/mL	4 mg/mL
S2921	PF-4981517	<1 mg/mL	91 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	Apigenin is a potent P450 inhibitor for CYP2C9 with IC50 of 23 pM
Targets
IC50
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]
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]
Clinical Trials
Features	Much more potent than kaempferol and myricetin in CT-L inhibition

Protocol(Only for Reference)

1

References

Chemical Information

Download Apigenin SDF

Molecular Weight (MW)	270.24
Formula	C₁₅H₁₀O₅
CAS No.	520-36-5
Synonyms	N/A

Solubility (25°C) DMSO 54 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Validation & Quality Control

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Related Compound Libraries

Apigenin is available in the following compound libraries:

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1250	MDV3100 (Enzalutamide)	<1 mg/mL	93 mg/mL	3 mg/mL
S2246	Abiraterone Acetate (CB7630)	<1 mg/mL	<1 mg/mL	28 mg/mL
S1190	Bicalutamide (Casodex)	<1 mg/mL	86 mg/mL	7 mg/mL
S1123	Abiraterone (CB-7598)	<1 mg/mL	0.33 mg/mL	<1 mg/mL
S2187	Avasimibe(CI-1011)	<1 mg/mL	100 mg/mL	8 mg/mL
S1442	Voriconazole	<1 mg/mL	70 mg/mL	20 mg/mL
S1353	Ketoconazole	<1 mg/mL	16 mg/mL	10 mg/mL
S1908	Flutamide (Eulexin)	<1 mg/mL	55 mg/mL	55 mg/mL
S2555	Clarithromycin (Biaxin, Klacid)	<1 mg/mL	18 mg/mL	<1 mg/mL
S2042	Cyproterone acetate	<1 mg/mL	≥83 mg/mL	≥10 mg/mL
S2803	Galeterone (TOK-001)	<1 mg/mL	24 mg/mL	40 mg/mL
S1195	TAK-700 (Orteronel)	<1 mg/mL	62 mg/mL	8 mg/mL
S2526	Alizarin	<1 mg/mL	48 mg/mL	<1 mg/mL
S2046	Pioglitazone HCl (Actos)	<1 mg/mL	79 mg/mL	4 mg/mL
S2921	PF-4981517	<1 mg/mL	91 mg/mL	<1 mg/mL

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Apigenin

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Apigenin is available in the following compound libraries:

Product Information

Compare P450 (e.g. CYP17) Inhibitors

Product Description

Biological Activity

Protocol(Only for Reference)

References

Chemical Information

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Related P450 (e.g. CYP17) Inhibitors

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