Go 6983

Catalog No.S2911 Synonyms: GOE 6983

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  
In DMSO USD 250 In stock
USD 190 In stock
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3 Customer Reviews

  • (a) In vitro kinase reactions were performed by using GSTp531-64 (FP267) as substrate and GST-CK1δ (FP449) as enzyme, or using (b) GST-CK1δ375–428 (FP1183) as substrate and recombinant PKCα as enzyme in combination with one of three PKC-specific inhibitors (Go-6983, enzastaurin, and bisindolylmaleimide I (BIM I), respectively). Data are presented as normalized bar graph.

    Amino Acids, 2016, 48(5):1185-97. Go 6983 purchased from Selleck.

    MC3T3-E1 cells were transfected with pcDNA3-CFP-CITED1 and cultured for 48 h. Thereafter, cells were cultured in α-MEM with 1% FBS for 12 h; the medium was then replaced with Hank's solution+α-MEM (ratio=8:2) and cultured for another 20 min. 1 μM Go6983 or vehicle were cultured for 1 h before 100 nM hPTH treatment. 10 μM Phorbol ester (TPA) was applied to the cells for 30 min.

    Cellular Signalling, 2014, 26(11): 2436-2445. Go 6983 purchased from Selleck.

  • Immunoblot analysis and quantitative analysis of pPKC, Claudin-1, ZEB1, ZO-1, Slug, Twist, MMP9 after treatment with 1μM Go 6983 in 231 HM STC2i cells at different time point.

    PLoS One, 2015, 10(4): e0122179 . Go 6983 purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

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]

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]

+ Expand
  • Animal Models: Mice bearing B16BL6 tumors
  • Formulation: PBS
  • 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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

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Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID