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Go 6983

Cat. No. M2019
Go 6983 Structure
Synonym:

Goe 6983

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 87  USD87 In stock
10mg USD 155  USD155 In stock
50mg USD 485  USD485 In stock
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Quality Control
Biological Activity

Go 6983 is a protein kinase C (PKC) inhibitor with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCζ respectively. Go 6983 inhibited intracellular Ca(2+) accumulation, suggesting a mechanism for its vasodilator properties. In vitro, Go 6983 significantly inhibited antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 (100 nM) significantly reduced PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts (P < 0.01), and significantly inhibited superoxide release from PMNs by 90 +/- 2% (P < 0.01). Go 6983 attenuated post-I/R cardiac contractile dysfunction, which may be related in part to decreased superoxide production in the presence of PMNs.

Customer Product Validations & Biological Datas
Source Immunobiology (2012). Figure 4. Go 6983
Method Flow cytometry
Cell Lines Tca8113 cells
Concentrations 5 μM
Incubation Time 24 h
Results As shown in Fig. 4, after PKD2 was inhibited by Gö6983, IFN-γ could not induce the surface expression of PD-L1 on Tca8113.
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 442.51
Formula C26H26N4O3
CAS Number 133053-19-7
Purity 99.94%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
References

[1] Young LH, et al. Cardiovasc Drug Rev. Gö 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury.

[2] Chen J, et al. Mol Pharmacol. Protein kinase C-independent effects of protein kinase D3 in glucose transport in L6 myotubes.

[3] Peterman EE, et al. J Cardiovasc Pharmacol. Gö 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Go 6983, Goe 6983 supplier, PKC, inhibitors

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