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 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).|
|Incubation time||48 hours|
|Animal models||LPS/D-GalN-challenged mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Gö 6976 is a potent inhibitor of neurotrophin-receptor intrinsic tyrosine kinase.
Behrens MM, et al. J Neurochem. 1999 Mar;72(3):919-24. PMID: 10037462.
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