KT5823

Names

[ Name ]:
KT5823

[Synonym ]:
MFCD00132119
(9S,10R,12R)-2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-l][1,6]benzodiazocine-10-carboxylic acid methyl ester

Biological Activity

[Description]:

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[1]. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression, and iodide uptake in thyroid cells[2]. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation[3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA

Research Areas >> Others

Signaling Pathways >> Stem Cell/Wnt >> PKA

Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

PKA:10 μM (Ki)

PKC:4 μM (Ki)

[References]

[1]. 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.

Chemical & Physical Properties

[ Density]:
1.52g/cm3

[ Boiling Point ]:
629.2ºC at 760mmHg

[ Molecular Formula ]:
C₂₉H₂₅N₃O₅

[ Molecular Weight ]:
495.52600

[ Flash Point ]:
334.3ºC

[ Exact Mass ]:
495.17900

[ PSA ]:
74.93000

[ LogP ]:
4.58930

[ Vapour Pressure ]:
9.67E-16mmHg at 25°C

[ Index of Refraction ]:
1.763

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Brain natriuretic peptide constitutively downregulates P2X3 receptors by controlling their phosphorylation state and membrane localization.

Mol. Pain 11 , 71, (2015)

ATP-gated P2X3 receptors are important transducers of nociceptive stimuli and are almost exclusively expressed by sensory ganglion neurons. In mouse trigeminal ganglion (TG), P2X3 receptor function is...

Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells.

Am. J. Physiol. Cell Physiol. 303(12) , C1260-8, (2012)

In this study, the interaction of natriuretic peptides (NP) and bradykinin (BK) signaling pathways was identified by measuring membrane potential (V(m)) and intracellular Ca(2+) using the patch-clamp ...

Cytoprotective effect of 1-nitro-2-phenylethane in mice pancreatic acinar cells subjected to taurocholate: putative role of guanylyl cyclase-derived 8-nitro-cyclic-GMP.

Biochem. Pharmacol. 91(2) , 191-201, (2014)

The nitroderivative 1-nitro-2-phenylethane (NPE) was recently described as a compound possessing heme-dependent soluble guanylyl cyclase (sGC) stimulating properties in vascular smooth muscle cells. I...