KT 5720 is prepared by a modificiation of K-252a , which is synthesized by the fungus Nocardiopsis sp. KT 5720 is a potent, specific and cell-permeable inhibitor of PKA (K_i = 56 nM). This compound blocks PKA signaling through competitive inhibition. KT 5720 does not affect the activity of other kinases, including pKC, pKG, or MLCK and can inhibit axon branching in cultured neurons. KT 5720 has been shown to reversibly arrest human skin fibroblasts in the G₁ phase of the cell cycle and regulate multiple signal transduction events vis-a-vis protein phosphorylation and cellular responses involving the cyclic AMP messenger system. This compound reversed suppression of mistletoe lectin II (MLII) by dibutyl-cAMP in HL-60 cells. KT 5720 shows inhibitor effects on PHK, PDK1, MEK, MSK1, Akt1 (PKBα) and GSK3β.

Nocardiopsissp. soil fungi, semi-synthetic

A potent, specific and cell-permeable inhibitor of PKA

≥97%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Solid

KT-5720

1.50 g/cm³ (Predicted)

714.96° C at 760 mmHg (Predicted)

n²⁰_D 1.75 (Predicted)

PHK: IC₅₀ = 0.01 µM (rabbit skeletal muscle); PDK1: IC₅₀ = 0.3 µM (His-tagged human)

PKA: K_i= 56 nM

Soluble in water (700 mg/L at 25 °C), chloroform (44.51 g/100mL at 25 °C), dichloromethane (19.20 g/100mL at 25 °C), methanol (9.98 g/100mL at 25 °C), DMSO (50 mM), ethanol (1.28 g/100mL at 25 °C)

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