Cat #: K-250
Lyophilized Powder yes
Every lot is tried & tested in a relevant biological assay.
Origin Nocardiopsis sp. (soil fungi).
Effective concentration 500 nM - 1 µM.
Chemical name (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-methoxy-2,9-di methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-k l]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester.
Molecular formula C29H25N3O5.
CAS No.: 126643-37-6
Activity KT5823 is a selective and potent inhibitor of PKG (IC50 = 234 nM)1,2.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to one week at 4°C or three months at -20°C.
- Alomone Labs KT5823 inhibits PLCβ3 phosphorylation via PKG in C6 glioma cells.Cells were grown to 70% confluence, and then serum starved for 18 h. The cells were then preincubated for 30 min in different concentrations of KT5823 (#K-250) and stimulated with 8Br-cGMP (100 µM, 4h, 37°C) for PKG activation. Cell proteins were resolved by SDS-PAGE and probed with anti phospho-PLCβ3. PLCβ3 is a substrate of PKG.
References - Scientific background
- Kase, H. et al. (1987) B.B.R.C. 142, 436.
- Hidaka, H. and Kobayashi, R. (1992) Annu. Rev. Pharmacol. Toxicol. 32, 377.
- Chijiwa, T. et al. (1990) J. Biol. Chem. 265, 5267.
- Ruth, P. (1999) Pharmacol. Ther. 82, 355.
- Pfeifer, A. et al. (1998) EMBO J. 17, 3045.
- Chan, S.L, and Fiscus, R.R. (2003) Mol. Hum. Reprod. 12, 775.
Scientific background KT5823 is a semi-synthetic derivative of K525a.1 It is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50= 234 nM). KT5823 interferes at the level of the ATP binding site of the catalytic domain of PKG.2,3 The PKG are Ser/Thr protein kinase with broad substrate specificity, and expressed in; brain, smooth muscle cells, platelets, juxtaglomerular kidney cells, and endothelial cells.4,5 KT5823 triggered apoptotic DNA fragmentation in immortalized uterine epithelial cells, suggesting a regulatory role for PKG in the apoptotic process in these cells.6
Last update: 13/10/2022
KT5823 (#K-250) is a highly pure, semi-synthetic, and biologically active compound.
For research purposes only, not for human use
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