Home Metabolism P450 (e.g. CYP17) Inhibitor Apigenin

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Apigenin P450 (e.g. CYP17) Inhibitor

Kat.-Nr.: S2262

Apigenin ist ein potenter P450-Inhibitor für CYP2C9 mit einem Ki von 2 μM.
Apigenin P450 (e.g. CYP17) Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 270.24

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.73%
99.73

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
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
Klicken Sie hier, um weitere experimentelle Zellliniendaten anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 270.24 Formel

C15H10O5

Lagerung (Ab Erhaltdatum)
CAS-Nr. 520-36-5 SDF herunterladen Lagerung von Stammlösungen

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 54 mg/mL (199.82 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewicht-Rechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.

Wirkungsmechanismus (Mechanism of Action)

Eigenschaften
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.
Referenzen
  • [4] https://pubmed.ncbi.nlm.nih.gov/19441930/
  • [5] https://pubmed.ncbi.nlm.nih.gov/25859163/
  • [6] https://pubmed.ncbi.nlm.nih.gov/24067903/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot MHC / MHC2A / MHC2B / MyoD CXCR4 CDK1 / Cyclin B1 / p21
S2262-WB1
29108230
Immunofluorescence E-caherin / Vimentin Snail
S2262-IF1
27203387
Growth inhibition assay Cell viability
S2262-viability1
23224239