Go6976

Catalog No.S7119 Synonyms: PD406976

Go6976 Chemical Structure

Molecular Weight(MW): 377.42

Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

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Cited by 10 Publications

5 Customer Reviews

  • Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.

    Cell Signal, 2016, 28(9):1422-31.. Go6976 purchased from Selleck.

    Go6976 abolished the anticalcification activity of CST by promoting the ossification of cultured VSMCs. Rat VSMCs werecultured in growth medium or calcification medium in the presence or absence of 10 7mol/L of CST or in calcification medium containing10 7mol/L of CST and pretreated with different doses of Go6976 (0.01, 0.1 and 0.5lmol/L) for 30 min. On day 7 (A, n=4) and 12 (B,n=4), VSMCs were harvested for the determination of ALP activity (A) using an ALP assay kit and calcium content (B) using the OCPCmethod. The VSMCs cultured with calcification medium containing 10 7mol/L of CST were pretreated with different doses of Go6976 (0.01and 0.1lmol/L) for 30 min. On day 6, VSMCs were harvested for the detection of expression of OCN (C, D, n=6). Data from at least threeindependent experiments are presented as the mean SEM, and representative images are shown.*P<.05 and †P<.01. Ctrl, control groupin vitro;b-GP,b-glycerophosphate group;b-GP+CST,b-glycerophosphate plus 10 7mol/L cortistatin group;b-GP+CST+Go6976,b-glycerophosphate plus 10 7mol/L cortistatin plus Go6976 group.

    Acta Physiol, 2018, 223(3):e13055. Go6976 purchased from Selleck.

  • Representative micrographs showing immunostaining results for p-PKCα and laminin, LC3 and laminin, SQSTM1/p62 and laminin, LAMP2 and laminin in the kidneys at day 7 after UUO. Slides were counterstained with DAPI to visualize cell nuclei.

    J Biol Chem, 2018, doi:10.1074/jbc.RA118.002191. Go6976 purchased from Selleck.

    Inhibition of InlB-mediated entry by a chemical inhibitor of PKC-α. HeLa cells were treated with the indicated concentrations of the compound Go6976 699 or with the vehicle DMSO for 45 min before assessment of bacterial entry or cell viability. (i). The effect of Go6976 treatment on entry of Listeria expressing InlB is shown. Data are means +/- SEM from three experiments. *, P < 0.05 compared to the DMSO only (-) condition. (ii). Go6976 treatment did not affect viability of HeLa cells as measured with MTT assays. Results are mean +/- SEM values from three experiments. (iii). Go6976 treatment did not reduce entry of E. coli strain HB101 expressing the invasin protein of Yersinia enterocolitica (inv+ HB101). Data are mean +/- SEM values from three experiments.

    Infect Immun, 2017, e00087-17. Go6976 purchased from Selleck.

  • Upper: representative immunoblots of the total lysates of cultured astrocytes after SHH or BSA with or without Go6976 for 6h. Lower: statistics, n = 4 in each condition.

    Neuroscience, 2017, 365:217-225. Go6976 purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

Biological Activity

Description Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
Targets
JAK2 [2]
(Cell-free assay)
FLT3 [2]
(Cell-free assay)
PKCα [1]
(Cell-free assay)
PKCβ1 [1]
(Cell-free assay)
PKC [1]
(Rat brain)
2.3 nM 6.2 nM 7.9 nM
In vitro

Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. [1] Beside WT JAK2, Go6976 also inhibits the mutant forms (JAK2 V617F and TEL-JAK2) found in haematological malignancies, and has activity against mutant forms of FLT3. In AML cells, Go6976 reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples.[2] Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6. [3]

Assay
Methods Test Index PMID
Western blot
p-EGFR / EGFR / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 ; 

PubMed: 23229345     


Potency of Gö6976 in NCI-H1975 cells. Gö6976 treatment in NCI-H1975 at various concentrations for 3 hr. IC50 concentration for suppression of pEGFR is ~100 nM.

23229345
Immunofluorescence
p62 / LAMP2 ; 

PubMed: 29794026     


Representative images for SQSTM1/p62 and LAMP2 among different groups as indicated. Yellow dots in merged images represent colocalization of SQSTM1/p62 and LAMP2. Cells were co-stained with DAPI to visualize the nuclei; scale bar, 5 μm. Quantitative analysis for SQSTM1/p62 puncta/cell and merged dots/p62 in NRK-49F cells after various treatments is as indicated (lower part). *, p < 0.05; **, p < 0.01; ***, p < 0.001 compared with vehicle (Veh)-treated cells (n = 5–7); #, p < 0.05 compared with cells treated with Go6976. 

29794026
In vivo Go6976 (2.5 mg/kg i.p.), as a PKD inhibitor, effectively prevents LPS/D: -GalN-induced acute liver injury by inhibition of MAPKs activation to reduce TNF-α production, and significantly improves the survival of LPS/D-GalN-challenged mice. [4]

Protocol

Kinase Assay:

[1]

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PKC Activity Assay:

In brief, for measuring PKCα, and PKCβ1 and PKC from rat brain, the assay mixture of 200 μl contains 50 mM HEPES (pH7.5), 5 mM MgCl2, 1 mM EDTA, 1.25 mM EGTA, 1.32 mM CaC12, 1 mM dithiothreitol, 1 μg of phosphatidylserine, 0.2 μg of diolein, 40 μg of histone Hi, 10 μM [γ-32P]ATP (1 μCi/ml), and 5-10 units (pmol of Pi/min) of PKC. Assays are started by the addition of [γ-32P]ATP, incubated for 5 min at 30 °C, stopped by the addition of 2 ml of 8.5% H3PO4, filtered through 0.45-μm nitrocellulose filters, and evaluated by scintillation counting.
Cell Research:

[2]

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  • Cell lines: Primary AML cells
  • Concentrations: 1 μM
  • Incubation Time: 48 hours
  • Method:

    Cells are suspended at 2 × 105 per point in 200 μl RPMI/10% FCS. The inhibitor under investigation is added at the appropriate concentration and the cells incubated for 48 h at 37°C, 5% CO2. MTS activity is measured by CellTiter kit according to the manufacturers instructions. Results are expressed as a percentage of control (cells without inhibitor).


    (Only for Reference)
Animal Research:

[4]

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  • Animal Models: LPS/D-GalN-challenged mice
  • Formulation: DMSO
  • Dosages: 2.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL warmed (47.69 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na+1% Tween 80
For best results, use promptly after mixing.
30mg/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 377.42
Formula

C24H18N4O

CAS No. 136194-77-9
Storage powder
in solvent
Synonyms PD406976

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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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PKC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID