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Biological Activity:

Go6983 is a potent pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM,10 nM and 60 nM, respectively. It is inactive to PKCμ. Go6983 displays cardioprotective properties. It can reduce polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury. It can also optimize na?ve human pluripotent stem cell growth and viability following na?ve cell derivation from primed ESCs and iPSCs using na?ve human stem cell medium (NHSM). It is used in a chemical cocktail of seven small molecules to directly convert human fibroblasts into neuronal cells bypassing a neural progenitor stage.

How to Use:

In vitro: Go6983 was used at 1-5 μM final concentration in vitro and in cellular assays.
In vivo: Go6983 was dosed by IV injection to mice bearing B16BL6 tumors at 22 μg per mouse.

Reference:

• 1. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. (1996) FEBS Lett. 392(2):77-80.
• 2. Peterman EE, et al. G? 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. (2004) J Cardiovasc Pharmacol. 43(5):645-56.
• 3. Young LH, et al. G? 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. (2005) Cardiovasc Drug Rev. 23(3):255-72.
• 4. Gafni O, et al. Derivation of novel human ground state naive pluripotent stem cells. (2013) Nature. 504(7479):282-6.?
• 5. Hu W, et al. Direct Conversion of Normal and Alzheimer's Disease Human Fibroblasts into Neuronal Cells by Small Molecules. (2015) Cell Stem Cell. 17(2):204-12.?