Go 6983

For research use only.

Catalog No.S2911 Synonyms: GOE 6983

41 publications

Go 6983 Chemical Structure

Molecular Weight(MW): 442.51

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 250 In stock
USD 190 In stock
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Selleck's Go 6983 has been cited by 41 publications

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Biological Activity

Description Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.
Targets
PKCγ [1]
(Cell-free assay)
PKCα [1]
(Cell-free assay)
PKCβ [1]
(Cell-free assay)
PKCδ [1]
(Cell-free assay)
PKCζ [1]
(Cell-free assay)
6 nM 7 nM 7 nM 10 nM 60 nM
In vitro

Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. [1] In hearts reperfused with PMNs and Gö 6983 (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. Gö 6983 (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%. Gö 6983 attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. [2] Gö 6983 significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. [3] Go-6983 (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. [4] Go 6983 is isoform-specific PKC inhibitor that target the ATP binding site. Go 6983 inhibits ΔPfPKB activity with an IC50 of 1 μM. In Go 6983 (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. Go 6983 (5 μM) treatment results in an almost 60% decrease in formation of new rings in P. falciparum cultures. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MYXGeY5kfGmxbjDhd5NigQ>? MoDONVAh|ryP M3n5[VEhcA>? MYjtZZJs\WSueTDpcohq[mm2ZXSgRXRR|rOVLYP0bY12dGG2ZXSgUmFFWEhib4jp[IF{\SCjY4Tpeol1gSCjbnSgTFJQOiCjbnSvc5IhWk:VIHflcoVz[XSrb36= MVmyN|MzPjV6Mx?=
HeLa M1X2NWZ2dmO2aX;uJIF{e2G7 NXXUbHh7OiEQvF2= NX7Od41RPDhiaB?= NXfCdmZZe3WycILld5Nm\CC2aHWg[YZn\WO2IH;mJHBOSSCxbjDhdIlkfWyjcnXuJGEucW6mdXPl[EBkgXSxdH;4bYNqfHl? M3uzTlI1PDR5M{O5
Caco-2 NUDacYdDTnWwY4Tpc44h[XO|YYm= NXL5ZmdPOiEQvF2= MnzHPEBp NEDxdGZkd22ybHX0[Yx6KGG2dHXueYF1\WRiUF3BMYlv\HWlZXSgSmxKWCCvUl7BJIV5eHKnc4Ppc44> NVzHflF{OTZyNUK1NVY>
KM12C NVPiWGpyTnWwY4Tpc44h[XO|YYm= M17KW|Ih|ryP NGfweVY5KGh? NWDTOnVS[XS2ZX71ZZRm\CCSTVGtbY5lfWOnZDDGUGlRKG2UTlGg[ZhxemW|c3nvci=> MVOxOlA2OjVzNh?=
KM20 MYDGeY5kfGmxbjDhd5NigQ>? NXfpUYlvOiEQvF2= MYW4JIg> M{HjbYF1fGWwdXH0[YQhWE2DLXnu[JVk\WRiRlzJVEBuWk6DIHX4dJJme3Orb36= NV36ZWdQOTZyNUK1NVY>
HT29 NWHo[G9FTnWwY4Tpc44h[XO|YYm= MVSyJO69VQ>? MmnnPEBp M2DwNYF1fGWwdXH0[YQhWE2DLXnu[JVk\WRiRlzJVEBuWk6DIHX4dJJme3Orb36= Mn:3NVYxPTJ3MU[=
HCT116 M1fT[2Z2dmO2aX;uJIF{e2G7 NIG0PJYzKM7:TR?= NEi5flY5KGh? MnjTZZR1\W63YYTl[EBRVUFvaX7keYNm\CCITFnQJI1TVkFiZYjwdoV{e2mxbh?= MVOxOlA2OjVzNh?=
PC-3 NH7D[HBHfW6ldHnvckBie3OjeR?= NE\iWlQyKM7:TR?= NEfsS|YzKGh? NFznTYhIy7Z4OUizJIFjem:pYYTld{B1cGViVGDBMYlv\HWlZXSgVmdHWiC2cnHud4FkfGm4YYTpc44hemW|cH;ud4U> MV[xOVg6PzJ|Nh?=
PC12 Ml\sSpVv[3Srb36gZZN{[Xl? MojNNE42KM7:TR?= M1r5[2dQPjl6MzDicI9kc2WmIITo[UBm\m[nY4Sgc4YhWE2DIH;uJJRp\SCjY4TpeoF1cW:wIH;mJGFsfCCjbnSgUWFRUyCrbnT1Z4VlKGK7IFnHSk0y MWWxNFc5QDR2Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PKCη / PKCα / PKCδ / PKCε ; 

PubMed: 22892130     


MCF-7 cells were treated with 1 μM Gö 6983 for 15 h. Total cell lysates were subjected to SDS-PAGE and Western blot analysis was performed using the indicated antibodies. 

22892130
In vivo Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model. [6]

Protocol

Animal Research:

[6]

- Collapse
  • Animal Models: Mice bearing B16BL6 tumors
  • Dosages: 22 μg/mouse
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 59 mg/mL (133.33 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 442.51
Formula

C26H26N4O3

CAS No. 133053-19-7
Storage powder
in solvent
Synonyms GOE 6983
Smiles COC1=CC=C2[N](CCCN(C)C)C=C(C2=C1)C3=C(C(=O)NC3=O)C4=C[NH]C5=C4C=CC=C5

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID