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

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.79%

99.79

Relaterade mål	TGF-beta/Smad ROCK Bcr-Abl
Övrigt PKC Inhibitorer	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

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning	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
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	442.51	Formel	C₂₆H₂₆N₄O₃	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	133053-19-7	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	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

Löslighet (Solubility)

In vitro
Batch:

DMSO : 89 mg/mL (201.12 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (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.
Kinasanalys	Bindningsanalys
Kinasanalys	Fosforyleringsreaktioner utförs i en total volym av 100 μL innehållande buffert C (50 mM Tris-HC1, pH 7.5, 10 mM β-merkaptoetanol), 4 mM MgCl₂, 10 μg PS, 100 nM TPA, 5 μL av ett Sf158-cellextrakt som källa till rekombinant PKCμ eller av Sf9-cellextrakt som källa till andra rekombinanta PKC-isoenzymer, 10 μg syntide 2 som substrat, samt 35 μM ATP innehållande 1 μCi [γ-³²P]ATP. I vissa experiment utelämnas PS och TPA eller så tillsätts olika hämmare i koncentrationer som anges i texten. Efter inkubering i 10 min vid 30℃ avbryts reaktionen genom att 50 μL av analysblandningen överförs till en 20 mm kvadratisk bit fosfocellulosapapper, som tvättas 3 gånger i avjoniserat vatten och två gånger i aceton. Radioaktiviteten på varje papper bestäms genom vätskescintillationsräkning.
In vivo	Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model.
Referenser	[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/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	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 Hämmare

Molekylvikt: 442.51

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Go 6983 PKC Hämmare

Molekylvikt: 442.51

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)