KT5823
- Product Name
- KT5823
- CAS No.
- 126643-37-6
- Chemical Name
- KT5823
- Synonyms
- KT5823;KT 5283;KT5823;KT-5823;KT5823, inhibitor of PKG;PROTEIN KINASE INHIBITOR KT 5823;KT5823 - CAS 126643-37-6 - Calbiochem;9-Methoxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epxoy-1H,8H,11H-2,7B-11A-triazadibenzo(A,G)cycloocta(cde)-trinden-1-one;(9R)-2,3,9,10,11,12-Hexahydro-10β-methoxy-2,9-dimethyl-1-oxo-9α,12α-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester;(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-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester;(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-I][1,6]BENZODIAZOCINE-10-CARBOXYLIC ACID, METHYL ESTER
- CBNumber
- CB7377637
- Molecular Formula
- C29H25N3O5
- Formula Weight
- 495.53
- MOL File
- 126643-37-6.mol
KT5823 Property
- Boiling point:
- 629.2±55.0 °C(Predicted)
- Density
- 1.52±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- ethyl acetate: 5 mg/mL
- form
- lyophilized powder
- pka
- -1.01±0.60(Predicted)
- color
- white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
N-Bromosuccinimide Price
- Product number
- 420321
- Product name
- KT5823 - CAS 126643-37-6 - Calbiochem
- Purity
- Highly specific, cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase G (Ki = 234 nM).
- Packaging
- 50μg
- Price
- $159
- Updated
- 2024/03/01
- Product number
- K1388
- Product name
- KT 5823
- Purity
- ≥85% (HPLC), lyophilized powder
- Packaging
- 100μg
- Price
- $219
- Updated
- 2024/03/01
- Product number
- 420321
- Product name
- KT5823 - CAS 126643-37-6 - Calbiochem
- Purity
- Highly specific, cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase G (Ki = 234 nM).
- Packaging
- 100μg
- Price
- $259
- Updated
- 2024/03/01
- Product number
- 10010965
- Product name
- KT 5823
- Purity
- ≥95%
- Packaging
- 25μg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 10010965
- Product name
- KT 5823
- Purity
- ≥95%
- Packaging
- 50μg
- Price
- $68
- Updated
- 2024/03/01
KT5823 Chemical Properties,Usage,Production
Description
KT5823 (126643-37-6) is a selective protein kinase G inhibitor (K>i =0.23, 4 and >10 μM for PKG, PKC and PKA respectively.1?Arrests human skin fibroblast cell cycle after the G0/G1 boundary.2 KT5823 abolishes the cGMP-induced relaxation in smooth muscle cells (IC50=60 nM).3?Cell permeable.
Chemical Properties
Yellow powder
Uses
KT 5823 is a protein kinase inhibitor shown to increase TSH-induced NIS expression, and thus iodide uptake, in thyroid cells.
Uses
KT 5823 has been used as cyclic guanosine monophosphate (cGMP)-dependent protein kinase (PKG) inhibitor in cortical cultures, cortical neurons and in mouse brain capillary endothelial cells.
Definition
ChEBI: KT 5823 is an organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of methyl (3R)-3-methoxy-2-methyltetrahydrofuran-3-carboxylate (the 2S,3R,5R product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1-methyl-1,5-dihydro-2H-pyrrol-2-one. It has a role as an EC 2.7.11.12 (cGMP-dependent protein kinase) inhibitor. It is a gamma-lactam, an organic heterooctacyclic compound, a methyl ester, a hemiaminal and an indolocarbazole.
General Description
Highly specific cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase G (Ki = 234 nM). Inhibits protein kinase C (Ki = 4.0 μM) and protein kinase A (Ki >10.0 μM) at higher concentrations.
Biological Activity
Selective inhibitor of protein kinase G (K i values are 0.23, 4 and > 10 μ M for inhibition of PKG, PKC and PKA respectively). Inhibits SNP-stimulated PKG activity with an IC 50 of 60 nM in dispersed smooth muscle cells and has little effect on PKA activity at concentrations of up to 10 μ M. Also available as part of the Mixed Kinase Inhibitor Tocriset™ .
Biochem/physiol Actions
Cell permeable: yes
storage
-20°C (desiccate)
References
1) Kase et al. (1987), K252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436 2) Gadbois et al. (1992), Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells; Proc. Natl. Acad. Sci. USA, 89 8626 3) Murthy et al. (1995), Interaction of cA-kinase and cG-kinase in mediating relaxation of dispersed smooth muscle cells; Am. J. Physiol., 268 C171
KT5823 Preparation Products And Raw materials
Raw materials
Preparation Products
KT5823 Suppliers
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