KT5823

KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki 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].

Product Specifications

CAS Number

[126643-37-6]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Antibiotic; Apoptosis; Bacterial; PKA; PKC

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Epigenetics; Stem Cell/Wnt; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/kt5823.html

Purity

99.90

Solubility

DMSO : ≥ 20mg/mL

Smiles

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

Molecular Formula

C29H25N3O5

Molecular Weight

495.53

Precautions

H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.|[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.