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Go6976 selectively inhibits PKCα and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively). Go6976 also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC50 values are 5, 30, 130 and 370 nM respectively), PKCμ (PKD1) and the mitotic spindle checkpoint. Go 6976 blocks neurotrophin-induced signaling and autophosphorylation of neurotrophin-specific tyrosine kinase (Trk) receptors.
| Cell Experiment | |
|---|---|
| Cell lines | Primary AML cells |
| Preparation method | Suspending cells at 2 × 105 per point in 200 μl RPMI/10% FCS. Adding the inhibitor under investigation at the appropriate concentration and incubating the cells for 48 h at 37°C, 5% CO2. Measuring MTS activity by CellTiter kit according to the manufacturers instructions. Expressing results as a percentage of control (cells without inhibitor). |
| Concentrations | 1 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | LPS/D-GalN-challenged mice |
| Formulation | DMSO |
| Dosages | 2.5 mg/kg |
| Administration | i.p. |
| Molecular Weight | 378.43 |
| Formula | C24H18N4O |
| CAS Number | 136194-77-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PKC Products |
|---|
| Sapintoxin D
Sapintoxin D is a fluorescent phorbol ester that can be used to study the activation of protein kinase C (PKC). |
| Bryostatin 3
Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. |
| Ruboxistaurin mesylate
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. |
| PKC β pseudosubstrate
PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC. |
| Protein Kinase C (19-31)
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), is used as protein kinase C substrate peptide for testing the protein kinase C activity. |
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