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Stock availabilitIn Stock
In Stock
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CAS number
126643-37-6
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Description
PKG kinase inhibitor
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Molecular weight
495,5 g/mol
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Primary research fields
Cell Signaling, Cancer, Apoptosis, Cancer Growth Inhibitors, Tyrosine Kinase Inhibitors
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Other name
(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
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Product category
Small Molecules
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Product type
Inhibitor
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Chemical formula
C29H25N3O5
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Origin
Synthetic
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Purity pourcentage
≥98% (TLC)
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Soluble in
Soluble in DMSO (20 mg/ml), dimethyl formamide (20 mg/ml) and ethyl acetate (5 mg/ml)
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Physical appearance
White solid
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Storage recommendations
-20ºC
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Shipping recommendations
Shipped Ambient
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Safety information
Classification: Not a hazardous substance or mixture. Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection.
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PubChem number
3843
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Scientific context
KT5823 is a potent, selective, and reversible inhibitor of Protein Kinase G (PKG). It is a derivative of K-252a. KT5823 has been shown to inhibit SNP-stimulated PKG activity in dispersed smooth muscle cells. It has also been observed to dose-dependently inhibit spontaneous apoptosis of neutrophils.
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Bibliography
1. Murthy K.S., & Makhlouf G.M. (1995) Am J. Phys. 268(1 Pt 1): C171–180. 2. Brunetti M., et al. (2002) Biochem. Biophys. Res. Comm. 297(3): 498–501. 3. Kase H., et al. (1987) Biochem. Biophys. Res. Comm. 142(2): 436–440.
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Release date
1-Oct-2014
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PubMed number
Refer to PubMed
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Tested applications
To be tested
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Tested reactivity
To be tested
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Representative figure legend
Chemical structure of KT 5823 (SIH-458), a PKG kinase inhibitor. CAS #: 126643-37-6. Molecular Formula: C29H25N3O5. Molecular Weight: 495.5 g/mol. Chemical structure of KT 5823, a PKG kinase inhibitor (SIH-458). CAS # 126643-37-6. Molecular Formula: C29H25N3O5.
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Warning information
Non-hazardous
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Country of production
Canada
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Total weight kg
0.25
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Net weight g
0.0001
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.