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KT5823

Product Name
KT5823
CAS No.
126643-37-6
Chemical Name
KT5823
Synonyms
KT5823;KT 5283;KT5823;KT-5823;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;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-, methyl ester, (9S,10R,12R)-
CBNumber
CB7377637
Molecular Formula
C29H25N3O5
Formula Weight
495.53
MOL File
126643-37-6.mol
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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.
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Safety

Hazard Codes 
Xi
WGK Germany 
3
F 
10
HS Code 
29349990
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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.

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N-Bromosuccinimide Price

Sigma-Aldrich
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
Sigma-Aldrich
Product number
K1388
Product name
KT 5823
Purity
≥85% (HPLC), lyophilized powder
Packaging
100μg
Price
$219
Updated
2024/03/01
Sigma-Aldrich
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
Cayman Chemical
Product number
10010965
Product name
KT 5823
Purity
≥95%
Packaging
25μg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
10010965
Product name
KT 5823
Purity
≥95%
Packaging
50μg
Price
$68
Updated
2024/03/01
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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

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KT5823 Suppliers

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126643-37-6, KT5823Related Search:

ZM 336372 STO-609 (acetate) Sunitinib Malate GW5074 ANTI-ANDROGEN RECEPTOR KT5823 (semi-synthetic derivative of K525a), Selective PKG Inhibitor, 0.4955kD KT5823 (Selective PKG Inhibitor) 11,12-Dihydroindolo[2,3-a]carbazole Lestaurtinib 9-CARBAZOLEPROPIONIC ACID K-252C KT5823 1-(1-METHYL-1H-INDOL-4-YL)METHYLAMINE 97 9-ISOPROPYLCARBAZOLE K-252A CARBAZOL-9-YL-METHANOL

  • PROTEIN KINASE INHIBITOR KT 5823
  • 9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-, methyl ester, (9S,10R,12R)-
  • (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
  • KT5823
  • (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
  • (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
  • 9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-, methyl ester, (9R-(9alpha,10beta,12alpha))-
  • 9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-, methyl ester, (9R,10R,12R)-
  • 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
  • KT 5283
  • KT5823;KT-5823
  • KT5823 - CAS 126643-37-6 - Calbiochem
  • 126643-37-6
  • C29H25N3O5
  • BioChemical
  • Cell Biology
  • Cell Signaling and Neuroscience
  • Serine/Threonine Kinase Inhibitors
  • Kinase/Phosphatase Biology
  • Protein Kinase G (PKG)
  • Cyclic Nucleotide related
  • antibiotic
  • Protein Kinase G (PKG)Cell Signaling and Neuroscience
  • Enzyme Inhibitors by Enzyme
  • Kinase/Phosphatase Biology
  • P to
  • Protein kinase CSerine/Threonine Kinase Biology
  • Protein Kinase Inhibitors
  • Serine/Threonine Kinase Inhibitors