Go6976 136194-77-9

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Molecular Weight:

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.


Biological Activity


Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. 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. Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6.


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.


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.

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).

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Product Categories : Protein Tyrosine Kinase > VEGFR Inhibitor