KT5823
Synonym(s):KT5823 - CAS 126643-37-6 - Calbiochem;PKG Inhibitor VII
- CAS NO.:126643-37-6
- Empirical Formula: C29H25N3O5
- Molecular Weight: 495.53
- MDL number: MFCD09878278
- EINECS: 603-150-0
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is KT5823?
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
The Uses of KT5823
KT 5823 is a protein kinase inhibitor shown to increase TSH-induced NIS expression, and thus iodide uptake, in thyroid cells.
The Uses of KT5823
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.
What are the applications of Application
KT5823 is a selective inhibitor of cGKI and spontaneous apoptosis
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
Properties of KT5823
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. |
Safety information for KT5823
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for KT5823
New Products
ALUMINIUM IODIDE 100 GM BUFFER CAPSULE PH 7.0 - 10 CAP BUFFER SOLUTION PH 9.5 (BORATE) EZEE BLUE GEL STAINER BORAX CARMINE (GRENACHERS ALCOHOLIC) POTASSIUM IODATE - IODIDE SOLN 0.1 N Dabigatran Acyl-O3-D-Glucuronide Trifluoroacetic Acid Salt Isofolic Acid Dabigatran 2-O-acylglucuronide metabolite Dabigatran Acyl-?-D- glucuronide Trifluroacetic Acid Erythromycin EP Impurity A Desloratidine Related Compound ARelated products of tetrahydrofuran
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