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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 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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Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
|Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
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