Name: Go 6983
Brand: Selleck Chemicals
SKU: S2911
Rating: 5 (97 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.79%

99.79

Gerelateerde doelwitten	TGF-beta/Smad ROCK Bcr-Abl
Overige PKC Inhibitoren	Darovasertib (LXS196) PMA chemical (Phorbol 12-myristate 13-acetate) Enzastaurin Sotrastaurin (AEB071) Bisindolylmaleimide I (GF109203X) Go 6976 Bisindolylmaleimide IX (Ro 31-8220) Mesylate Ruboxistaurin (LY333531) Hydrochloride Rottlerin PKC-theta inhibitor

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

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
PC12	Function assay	0.5 μM		GO6983 blocked the effect of PMA on the activation of Akt and MAPK induced by IGF-1	10788447
PC-3	Function assay	1 μM	2 h	Gö6983 abrogates the TPA-induced RGFR transactivation response	15897236
HCT116	Function assay	2 μM	8 h	attenuated PMA-induced FLIP mRNA expression	16052516
HT29	Function assay	2 μM	8 h	attenuated PMA-induced FLIP mRNA expression	16052516
KM20	Function assay	2 μM	8 h	attenuated PMA-induced FLIP mRNA expression	16052516
KM12C	Function assay	2 μM	8 h	attenuated PMA-induced FLIP mRNA expression	16052516
Caco-2	Function assay	2 μM	8 h	completely attenuated PMA-induced FLIP mRNA expression	16052516
A549	Function assay	10 μM	1 h	markedly inhibited ATPγS-stimulated NADPH oxidase activity and H2O2 and/or ROS generation	23326583
HeLa	Function assay	2 μM	48 h	suppressed the effect of PMA on apicularen A-induced cytotoxicity	24447339
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
HEK293	Function assay			Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in human HEK293 cells transfected with rabbit L-type calcium channel subunits, IC50 = 20 μM.	ChEMBL
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Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	442.51	Formule	C₂₆H₂₆N₄O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	133053-19-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	GOE 6983, Gö 6983			Smiles	CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 89 mg/mL (201.12 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.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	30.000mg/ml (67.80mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. 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.

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)

Targets/IC₅₀/Ki	PKCγ (Cell-free assay) 6 nM PKCα (Cell-free assay) 7 nM PKCβ (Cell-free assay) 7 nM PKCδ (Cell-free assay) 10 nM PKCζ (Cell-free assay) 60 nM
In vitro	Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. In hearts reperfused with PMNs and this compound (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values, respectively, significantly higher than PMNs alone. This chemical (100 nM) significantly reduces PMNs adherence to the endothelium and infiltration into the myocardium compared with Ischemia followed by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%. It attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. This inhibitor significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. It inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. This compound (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. It is isoform-specific PKC inhibitor that target the ATP binding site. It inhibits ΔPfPKB activity with an IC50 of 1 μM. In this chemical (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. This treatment (5 μM) results in an almost 60% decrease in formation of new rings in P. falciparum cultures.
Kinase Assay	Bindingsassay
Kinase Assay	Fosforyleringsreacties worden uitgevoerd in een totaal volume van 100 μL, bevattende buffer C (50 mM Tris-HC1, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl₂, 10 μg PS, 100 nM TPA, 5 μL van een Sf158-celextract als bron van recombinant PKCμ of van Sf9-celextracten als bron van andere recombinante PKC-iso-enzymen, 10 μg syntide 2 als substraat, en 35 μM ATP bevattende 1 μCi [γ-³²P]ATP. In sommige experimenten worden PS en TPA weggelaten of worden diverse remmers in de in de tekst aangegeven concentraties toegevoegd. Na incubatie gedurende 10 min bij 30℃, wordt de reactie beëindigd door 50 μL van het assay-mengsel over te brengen op een 20 mm vierkant stuk fosfocellulosepapier, dat 3 keer wordt gewassen in gedeïoniseerd water en twee keer in aceton. De radioactiviteit op elk papier wordt bepaald door vloeistofscintillatietelling.
In vivo	Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/8772178/ [2] https://pubmed.ncbi.nlm.nih.gov/15071351/ [3] https://pubmed.ncbi.nlm.nih.gov/16252018/ [4] https://pubmed.ncbi.nlm.nih.gov/11230348/ [5] https://pubmed.ncbi.nlm.nih.gov/15024016/ [6] https://pubmed.ncbi.nlm.nih.gov/19259669/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	PKCη / PKCα / PKCδ / PKCε		22892130

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Go 6983 PKC Remmer

Moleculair gewicht: 442.51

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)

Go 6983 PKC Remmer

Moleculair gewicht: 442.51

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)

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