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GSK650394 SGK inibitore

N. Cat.S7209

GSK650394 è un inibitore della chinasi-1 regolata dal siero e dai glucocorticoidi con IC50 di 62 nM e 103 nM rispettivamente per SGK1 e SGK2.

GSK650394 SGK inibitore Chemical Structure

Struttura chimica

Peso molecolare: 382.45

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Controllo Qualità

Lotto: Purezza: 99.92%

99.92

Target correlati	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Altro SGK Inibitori	EMD638683 PROTAC SGK3 degrader-1

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Descrizione dellattività
human M-1 cells	Function assay	Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment, IC50=0.58 μM
human MV-4-11 cell	Growth inhibition assay	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.1649 μM
human Daoy cell	Growth inhibition assay	Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.51532 μM
human BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=0.78455 μM
human KM12 cell	Growth inhibition assay	Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.85069 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.87937 μM
human RT-112 cell	Growth inhibition assay	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.02782 μM
human MONO-MAC-6 cell	Growth inhibition assay	Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=1.18097 μM
human HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.30172 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=1.30821 μM
human LCLC-97TM1 cell	Growth inhibition assay	Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=1.36768 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.40152 μM
human HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=1.42683 μM
human RKO cell	Growth inhibition assay	Inhibition of human RKO cell growth in a cell viability assay, IC50=1.57869 μM
human SNG-M cell	Growth inhibition assay	Inhibition of human SNG-M cell growth in a cell viability assay, IC50=1.79853 μM
human MCF7 cell	Growth inhibition assay	Inhibition of human MCF7 cell growth in a cell viability assay, IC50=1.8178 μM
human A431 cell	Growth inhibition assay	Inhibition of human A431 cell growth in a cell viability assay, IC50=1.85902 μM
human BC-3 cell	Growth inhibition assay	Inhibition of human BC-3 cell growth in a cell viability assay, IC50=1.87094 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=1.87611 μM
human SW620 cell	Growth inhibition assay	Inhibition of human SW620 cell growth in a cell viability assay, IC50=1.92816 μM
human HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=1.97312 μM
human MFH-ino cell	Growth inhibition assay	Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=1.98658 μM
human TE-12 cell	Growth inhibition assay	Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.99128 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.1871 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=2.19053 μM
human BC-1 cell	Growth inhibition assay	Inhibition of human BC-1 cell growth in a cell viability assay, IC50=2.51651 μM
human TE-15 cell	Growth inhibition assay	Inhibition of human TE-15 cell growth in a cell viability assay, IC50=2.59181 μM
human T84 cell	Growth inhibition assay	Inhibition of human T84 cell growth in a cell viability assay, IC50=2.60446 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.70082 μM
human CAL-12T cell	Growth inhibition assay	Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=2.71158 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.76731 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=2.78861 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=2.94825 μM
human EW-13 cell	Growth inhibition assay	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=3.01558 μM
human 5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM
human PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.33083 μM
human NCI-H2122 cell	Growth inhibition assay	Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=3.333 μM
human NCI-H460 cell	Growth inhibition assay	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=3.4041 μM
human CHL-1 cell	Growth inhibition assay	Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=3.49665 μM
human MOLT-16 cell	Growth inhibition assay	Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.51555 μM
human HCT-15 cell	Growth inhibition assay	Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=3.62842 μM
human G-361 cell	Growth inhibition assay	Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.71745 μM
human SK-LU-1 cell	Growth inhibition assay	Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.97014 μM
human ES4 cell	Growth inhibition assay	Inhibition of human ES4 cell growth in a cell viability assay, IC50=4.06069 μM
human TE-8 cell	Growth inhibition assay	Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.11582 μM
human IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=4.233 μM
human SW954 cell	Growth inhibition assay	Inhibition of human SW954 cell growth in a cell viability assay, IC50=4.46124 μM
human A375 cell	Growth inhibition assay	Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM
human CAL-27 cell	Growth inhibition assay	Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=5.33221 μM
human CAL-51 cell	Growth inhibition assay	Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=5.35583 μM
human SK-LMS-1 cell	Growth inhibition assay	Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=5.38255 μM
human HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=5.49347 μM
human NCI-H1299 cell	Growth inhibition assay	Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.98557 μM
human HT-29 cell	Growth inhibition assay	Inhibition of human HT-29 cell growth in a cell viability assay, IC50=7.26843 μM
human A388 cell	Growth inhibition assay	Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM
human SK-MEL-30 cell	Growth inhibition assay	Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=7.97215 μM
human CMK cell	Growth inhibition assay	Inhibition of human CMK cell growth in a cell viability assay, IC50=8.25377 μM
human HuP-T4 cell	Growth inhibition assay	Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=8.50234 μM
human SF126 cell	Growth inhibition assay	Inhibition of human SF126 cell growth in a cell viability assay, IC50=8.80208 μM
human MKN1 cell	Growth inhibition assay	Inhibition of human MKN1 cell growth in a cell viability assay, IC50=9.18565 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=9.91292 μM
human HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=10.68 μM
human SW872 cell	Growth inhibition assay	Inhibition of human SW872 cell growth in a cell viability assay, IC50=13.6896 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=13.7916 μM
human HuH-7 cell	Growth inhibition assay	Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=18.2783 μM
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=20.4955 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=21.2676 μM
human H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=21.4244 μM
human SK-MEL-3 cell	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=30.0228 μM
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	382.45	Formula	C₂₅H₂₂N₂O₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	890842-28-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			Smiles	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O

Solubilità

In vitro
Lotto:

DMSO : 76 mg/mL (198.71 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.500mg/ml (1.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 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 it; 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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	3.800mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 76 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.
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	SGK1 (Cell-free assay) 62 nM SGK2 (Cell-free assay) 103 nM
In vitro	GSK650394 inibisce il trasporto epiteliale mediato da SGK1 con un IC50 di 0,6 μM nel test SCC. Nelle cellule LNCaP, questo composto inibisce l'aumento della fosforilazione di Nedd4-2 mediato dagli androgeni e la crescita cellulare mediata dagli androgeni.Questa sostanza chimica contrasta la diminuzione della neurogenesi indotta dal cortisolo, i cambiamenti nella segnalazione Hedgehog e la traslocazione nucleare del GR. [2] Inibisce la replicazione del virus dell'influenza compromettendo l'esportazione delle vRNP dell'influenza nel citoplasma delle cellule A549.
Saggio chinasico	Test di prossimità a scintillazione (SPA)
Saggio chinasico	SGK1 S422D (60–431 aa; concentrazione finale 0,275 μg/mL) o SGK2 (concentrazione finale 0,875 μg/mL) sono attivati da PDK1 (concentrazione finale 1,1 μg/mL) in un tampone composto da 50 mM Tris (pH 7,5), 0,1 mM EGTA, 0,1 mM EDTA, 10 mM MgCl₂, 0,1% β-mercaptoetanolo, 1 mg/mL BSA e ATP (concentrazione finale di 0,15 mM) e incubato per 30 minuti a 30 °C. SGK2 è preparato esattamente come descritto per SGK1, tranne per il fatto che corrisponde alla proteina a lunghezza intera. Una soluzione contenente il peptide CROSStide biotinilato a una concentrazione finale di 75 μM e γ³²P-ATP corrispondente a 2×10⁶ cpm viene preparata nel tampone di reazione. In una piastra a 96 pozzetti, 5 μL di questo composto vengono aggiunti a 25 μL della miscela enzimatica attivata. Si aggiungono 20 μL della miscela CROSStide e si incuba per 1 ora a temperatura ambiente. Successivamente, si aggiungono 50 μL di una sospensione da 25 mg/mL di perline SPA rivestite di streptavidina in PBS con 0,1 M EDTA, pH 8,0. La piastra viene quindi sigillata e centrifugata per 8 minuti a 2000 rpm, e il segnale viene rilevato misurando per 30 secondi/pozzetto in un contatore a scintillazione Packard TopCount NXT. I valori IC50 dell'inibizione delle attività SGK1 e SGK2 da parte di questa sostanza chimica vengono calcolati da questi dati utilizzando il software GraphPad Prism 3.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/18794135/ [2] https://pubmed.ncbi.nlm.nih.gov/23650397/ [3] https://pubmed.ncbi.nlm.nih.gov/23487453/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	p-SGK2 / SGK2 p-SGK1 / SGK1 c-Jun / NRF2 p21 / LC3 / p62 / PARP / Cleaved PARP	26392083
Immunofluorescence	LC3	29017179
Growth inhibition assay	Cell viability	29017179

Supporto tecnico

Istruzioni per la manipolazione

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