KT5823

KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an K_i value of 0.23 μM, it also inhibits PKA and PKC with K_i values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na⁺/I^- symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation^{[1][2][3][4][5]}. IC50 & Target:Ki: 0.23 μM (PKG); 10 μM (PKG); 4 μM (PKG) (KT5823)^[1] In Vitro: KT5823 (15 μM, 18 h) arrests HSF55 cells in the G0 or G1 phase of the cell cycle^[3].
KT5823 (100 nM and 1 mM, 24 h) causes dose-dependent increases in apoptotic DNA fragmentation in unstressed HRE-H9 cells ^[3].
KT5823 (0.2-200 μM, 30 min) enhances 8-pCPT-cGMP (HY-137016)-induced VASP phosphorylation, but not inhibits the activation of PKA by Forskolin (HY-15371) in human platelets^[5].
In Vivo: KT5823 (2 nmol, i.c.v., a single dose for 14 days) blocks the ameliorating results of high-dose Bay 60-7550 (HY-14992) (3.0 mg/kg, i.p., a single dose for 14 days) both in long-term and short memories in the Aβ1-42-treated mice^[4].