Name: Apigenin
Brand: Selleck Chemicals
SKU: S2262
Rating: 5 (36 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.73%

99.73

Gerelateerde doelwitten	Dehydrogenase HSP Transferase PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Overige P450 (e.g. CYP17) Inhibitoren	Baicalein Naringenin Diosmetin Alizarin Orteronel Benzbromarone Sodium Danshensu Naringin Piperine Danshensu

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
mouse RAW264.7 cells	Function assay			Inhibition of COX2 protein expression in mouse RAW264.7 cells, IC50=0.5 μM
human H295R cells	Function assay			Inhibition of aromatase expressed in human H295R cells, IC50=1 μM
HEK293 FS cells	Function assay			Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.13 μM
human HeLa cells	Function assay			Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM
human MV4-11 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=2.81 μM
human mast cells	Function assay			Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=3 μM
MDCK cells	Function assay			Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=3.1 μM
human MDA-kb2 cells	Function assay			Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=5.2 μM
MCF-7 MX cells	Function assay			Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=5.9 μM
mouse RAW264.7 cells	Function assay		24 h	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method, IC50=6.7 μM
human H9 cells	Function assay		3 days	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=9 μM
HEK293 cells	Function assay		24 h	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=24.9 μM
mouse 26-L5 cells	Proliferation assay		72 h	Antiproliferative activity against mouse 26-L5 cells after 72 hrs by MTT assay, EC50=25 μM
human RS4:11 cells	Cytotoxicity assay		72 h	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=27.9 μM
mouse B16-BL6 cells	Proliferation assay		72 h	Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay, EC50=31.6 μM
human H9 cells	Cytotoxicity assay		3 days	Cytotoxicity against human H9 cells after 3 days, IC50=35 μM
human HT1080 cells	Proliferation assay		72 h	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay, IC
MDCK cells	Cytotoxicity assay			Cytotoxicity against MDCK cells by MTT assay, CC50=39.59 μM
mouse L929 cells	Function assay		15 mins	Potentiation of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining
human THP1 cells	Function assay	20 uM	1 h	Inhibition of NOX2 in human THP1 cells assessed as downregulation of TPA-induced CD36 mRNA expression at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis
MDA-MB-231 cells	Function assay	5 uM		Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	270.24	Formule	C₁₅H₁₀O₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	520-36-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 54 mg/mL (199.82 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.600mg/ml (5.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.800mg/ml (2.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Kenmerken	Much more potent than kaempferol and myricetin in CT-L inhibition.
Targets/IC₅₀/Ki	CYP2C9 2 μM(Ki)
In vitro	Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). This compound also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. It exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. It has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. This chemical suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. It 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. This compound blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. It 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. It 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. It is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. It inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. It inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. This compound also inhibits proliferating of human keratinocytes.
In vivo	Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. This compound inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. It 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. This chemical 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. This compound (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/9589348/ [2] https://pubmed.ncbi.nlm.nih.gov/20306120/ [3] https://pubmed.ncbi.nlm.nih.gov/17493651/ [4] https://pubmed.ncbi.nlm.nih.gov/19441930/ [5] https://pubmed.ncbi.nlm.nih.gov/25859163/ [6] https://pubmed.ncbi.nlm.nih.gov/24067903/

Toepassingen (Applications)

Methoden	Biomarkers	PMID
Western blot	MHC / MHC2A / MHC2B / MyoD CXCR4 CDK1 / Cyclin B1 / p21	29108230
Immunofluorescence	E-caherin / Vimentin Snail	27203387
Growth inhibition assay	Cell viability	23224239

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-07-01)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT07678749	ENROLLING_BY_INVITATION	Closed Sinus Lift; Apigenin Loaded Scaffold	Al-Azhar University	2025-11-05
NCT06889584	COMPLETED	Healthy	University of South Carolina	2025-02-15
NCT05788705	UNKNOWN	Rheumatoid Arthritis	Adel A.Gomaa	2023-07
NCT06560216	COMPLETED	Healthy	Chulalongkorn University	2024-10-28
NCT05999682	COMPLETED	Sepsis; Septic Shock	Zhujiang Hospital	2023-09-01	PHASE1; PHASE2
NCT05696665	UNKNOWN	Parkinson Disease; Neurodegenerative Diseases	Jinnah Postgraduate Medical Centre	2022-07-05

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Apigenin P450 (e.g. CYP17) Remmer

Moleculair gewicht: 270.24

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Apigenin P450 (e.g. CYP17) Remmer

Moleculair gewicht: 270.24

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)