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Isoliquiritigenin Aldose Reductase inhibitor

N. Cat.: S2404

Isoliquiritigenin, an anti-tumor flavonoid from the root of Glycyrrhiza glabra, inhibits aldose reductase with an IC50 of 320 nM.
Isoliquiritigenin Aldose Reductase inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 256.25

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.97%
99.97

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
KB cells Growth inhibition assay Compound concentration required to reduce the exponential growth of KB cells by 50%, CC50=12 μM
MT-4 cells Growth inhibition assay Compound concentration required to reduce the exponential growth of MT-4 cells by 50%, CC50=7.4 μM
Hepa lclc7 cells Cytotoxicity assay Cytotoxicity against mouse Hepa lclc7 cells, IC50=39 μM
J774.1 cells Function assay 24 h Inhibition of LPS-induced NO production in mouse J774.1 cells after 24 hrs by Griess reagent assay, IC50=29.3 μM
colon 26-L5 cells Cytotoxicity assay 72 h Cytotoxicity against mouse colon 26-L5 cells after 72 hrs by MTT assay, IC50=21.8 μM
MCF7 cells Cytotoxicity assay 25-150 μM 72 h Cytotoxicity against human MCF7 cells at 25 to 150 uM after 72 hrs by MTT assay
CHO cells Cytotoxicity assay Cytotoxicity against CHO cells by MTT assay, IC50=45.9 μM
human T47D cells Function assay 96 h Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay
MCF7 cells Function assay 96 h Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay
MCF7 cells Function assay Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay
mouse NIH3T3 cells Function assay 8 h Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay, IC50=4.8 μM
OE21 cells Cytotoxicity assay 72 h Cytotoxicity against human OE21 cells after 72 hrs by MTT assay, IC50=48 μM
U937 cells Function assay 5 ug/ml 24 h Antiinflammatory activity in human U937 cells assessed as inhibition of LPS-induced CCL5 secretion at 5 ug/ml after 24 hrs by ELISA relative to control
dog MDCK cells Function assay 20 ug/mL 1 h Antiviral activity against Influenza virus A/Puerto Rico/8/34 H1N1 infected in dog MDCK cells assessed as inhibition of viral replication at 20 ug/mL incubated at 1 hr post-infection measured after 24 hrs by hemagglutininating unit assay relative to control
dog MDCK cells Function assay 8 h Inhibition of PKC/p38MAPK-mediated nuclear-cytoplasmic viral ribonucleoprotein export in dog MDCK cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 8 hrs post-infection by inmmunofluorescence
NCI-H292 cells Function assay Inhibition of PKC-mediated PKD phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis
NCI-H292 cells Function assay Inhibition of PKC-mediated p38MAPK phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis
NCI-H292 cells Function assay Inhibition of PKC-mediated JNK phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis
dog MDCK cells Function assay Restoration of GSH level in dog MDCK cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 24 hrs post-infection by DTNB-based colometric assay
RBL-1 cells Function assay In vitro inhibition against 5-lipoxygenase in RBL-1 cells was determined, IC50=35 μM
PC3 cells Cytotoxicity assay Cytotoxicity against human PC3 cells, IC50=46.4 μM
HUVEC Cytotoxicity assay 48 h Toxicity against HUVEC incubated for 48 hrs by MTT assay, IC50=41.17 μM
K562 cells Cytotoxicity assay 48 h Antitumor activity against human K562 cells incubated for 48 hrs by MTT assay, IC50=29.27 μM
Hepa-1c1c7 cells Function assay Induction of quinone reductase activity in mouse Hepa-1c1c7 cells assessed as drug level required to double enzyme activity
Hepa lclc7 cells Function assay Induction of mouse quinone reductase in mouse Hepa lclc7 cells assessed as concentration required to double enzyme activity
U937 cells Function assay 5 ug/ml Inhibition of LPS-induced AP-1 activation in human U937 cells at 5 ug/ml after 1 hr relative to control
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 256.25 Formula

C15H12O4

 Conservazione (Dalla data di ricezione)
N. CAS 961-29-5 Scarica SDF Conservazione delle soluzioni stock

Sinonimi N/A Smiles C1=CC(=CC=C1C=CC(=O)C2=C(C=C(C=C2)O)O)O

Solubilità (Solubility)

In vitro
Lotto:

Ethanol : 26 mg/mL

DMSO : 12 mg/mL (46.82 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC50/Ki
Aldose reductase
(Cell-free assay)
320 nM
In vitro
Isoliquiritigenin may be effective in preventing diabetic complications through inhibiting rat lens aldose reductase with an IC50 of 320 nM and sorbitol accumulation in human red blood cells with an IC50 of 2.0 μM. This compound may also serve as a skin-lightening agent by inhibiting mono- and diphenolase tyrosinase activities with an IC50 of 8.1 μM. It induces cell cycle arrest and cell growth inhibition in DU145 and LNCaP prostate cancer cell lines. This chemical induces apoptosis of human gastric cancer MGC-803 cells through increasing the intracellular free calcium concentration and decreasing the mitochondrial transmembrane potential (Deltapsi(m)).
In vivo
LD50: Mice >6g/kg (i.g.)
Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/11731922/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19067384/