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Go6976

Cat. No. M3625
Go6976 Structure
Size Price Availability
5mg USD 135  USD150 Out of stock
25mg USD 342  USD380 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 378.43
Formula C24H18N4O
CAS Number 136194-77-9
Purity >98%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Go6976 supplier, PKC, inhibitors

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