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KN-93 phosphate is the water soluble form of KN-93. It is a potent, selective and cell permeable inhibitor of CaM kinase II (IC50= 0.37 μm, Ki=370 nm) [1]

CaMK II (calcium/calmodulin-dependent protein kinase II) is a multifunctional serine/threonine kinase with various roles in different physiological systems.

Since CaMK II can enhance cell proliferation, the CaMK II inhibitor KN-93 blocked the cell proliferation by regulating the expression of p53 and p21 in human hepatic stellate cells. [2] KN-93 inhibited the autophosphorylation of both α and β subunits of CaMK II. Moreover, KN-93 reduced dopamine level via modulating the TH reaction rate to reduce the Ca2+-mediated phosphorylation levels of the TH molecule in PC12h cells.[1] As CaMK II is necessary for cell cycle progression through G1, KN-93 also induced G1 cell cycle arrest and apoptosis in NIH 3T3 cells.[3]

In MRL/lpr Foxp3-GFP mice, KN-93 promoted the generation of Foxp3 regulatory T cells through the inhibition of CaMK IV in the spleen, peripheral lymph nodes and peripheral blood with decreased skin and kidney damage. [4] In a rat model of Parkinson's disease, intrastriatal injection of KN-93 relieved the levodopa-induced dyskinesia by suppressing the CaMK II activation. [5]

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