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]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

495.53

C₂₉H₂₅N₃O₅

126643-37-6

Solid

White to off-white

C[C@@]([C@@]1(OC)C(OC)=O)(O[C@](N2C3=C4C=CC=C3)([H])C1)N5C(C2=C4C6=C7CN(C)C6=O)=C7C8=C5C=CC=C8

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Gadbois DM, et al. Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells. Proc Natl Acad Sci U S A. 1992 Sep 15;89(18):8626-30.  [Content Brief]

  [2]. Wyatt TA, et al. KT5823 activates human neutrophils and fails to inhibit cGMP-dependent protein kinase phosphorylation of vimentin. Res Commun Chem Pathol Pharmacol. 1991 Oct;74(1):3-14.  [Content Brief]

  [3]. Chan SL, et al. Guanylyl cyclase inhibitors NS2028 and ODQ and protein kinase G (PKG) inhibitor KT5823 trigger apoptotic DNA fragmentation in immortalized uterine epithelial cells: anti-apoptotic effects of basal cGMP/PKG. Mol Hum Reprod. 2003 Dec;9(12):775-83.  [Content Brief]

  [4]. Ruan L, et al. Phosphodiesterase-2 Inhibitor Bay 60-7550 Ameliorates Aβ-Induced Cognitive and Memory Impairment via Regulation of the HPA Axis. Front Cell Neurosci. 2019 Oct 2;13:432.  [Content Brief]

  [5]. Burkhardt M, et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J Biol Chem. 2000 Oct 27;275(43):33536-41.  [Content Brief]