Home TGF-beta/Smad PKC inhibitor - FLT3 inhibitor - JAK inhibitor Go6976 For research use only.

Go6976

Synonyms: PD406976

Go6976 (PD406976) 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.

Go6976 Chemical Structure

Go6976 Chemical Structure

CAS No. 136194-77-9

Purity & Quality Control

Go6976 Related Products

Signaling Pathway

PKC Signaling Pathways

PKC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Vero Cytotoxicity assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis, CC50=6μM. 28689975
primary microglial cells Function assay Inhibition of IFN-gamma-induced IFN-gamma regulatory factor levels in Sprague-Dawley rat primary microglial cells by Western blotting 17395590
primary microglial cells Function assay 1.3 uM Suppression of IFN-gamma-induced PKCalpha/beta2 nuclear translocation in Sprague-Dawley rat primary microglial cells at 1.3 uM by Western blotting 17395590
primary microglial cells Function assay 1.3 uM Suppression of IFN-gamma-induced IFN-gamma regulatory factor 1 nuclear translocation in Sprague-Dawley rat primary microglial cells at 1.3 uM by Western blotting 17395590
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 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
Click to View More Cell Line Experimental Data

Biological Activity

Description Go6976 (PD406976) 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
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]
Kinase Assay 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 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).
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-EGFR / EGFR / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 23229345
Immunofluorescence p62 / LAMP2 29794026
In Vivo
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]
Animal Research Animal Models LPS/D-GalN-challenged mice
Dosages 2.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 377.42 Formula

C24H18N4O
CAS No. 136194-77-9 SDF Download Go6976 SDF
Smiles CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 44.7 mg/mL ( (118.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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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