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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
HS-243 HS-243 is a highly potent interleukin-1 receptor-associated kinase (IRAK) inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.
Targets
IRAK-4 (Cell-free assay); IRAK-1 (Cell-free assay); TAK1 (Cell-free assay) 20 nM; 24 nM; 0.5 μM
In vitro
HS-243 has exquisite selectivity toward both IRAK-1 (IC50 = 24 nM) and IRAK-4 (IC50 = 20 nM), with only minimal TAK1-inhibiting activity (IC50 = 0.5 μM). Using HS-243 and takinib, we evaluates the consequences of cytokine/chemokine responses after selective inhibition of IRAK-1/4 or TAK1 in response to lipopolysaccharide challenge in human rheumatoid arthritis fibroblast-like synoviocytes. HS-243 specifically inhibits intracellular IRAKs without TAK1 inhibition and these kinases have distinct, nonredundant signaling roles.
Cell Research(from reference)
Cell lines：RA-FLS cells, THP-1 cells
Concentrations：10 μM
Incubation Time：24 h
Umfassendes Dokument zu Gefahren, Handhabung, Lagerung und Einhaltung regulatorischer Vorschriften.
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Spezifikationsblatt ansehen →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Klasse | Benzimidazoles |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Benzimidazoles |
| Alternative Parents | Benzamides Nitrobenzenes Benzoyl derivatives Nitroaromatic compounds N-substituted imidazoles Heteroaromatic compounds Secondary carboxylic acid amides Propargyl-type 1,3-dipolar organic compounds Azacyclic compounds Organic oxoazanium compounds Organic oxides Hydrocarbon derivatives Organic salts Organic zwitterions Organonitrogen compounds Organooxygen compounds |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Benzamide - Benzimidazole - Benzoic acid or derivatives - Nitrobenzene - Nitroaromatic compound - Benzoyl - Monocyclic benzene moiety - N-substituted imidazole - Benzenoid - Azole - Heteroaromatic compound - Imidazole - Organic nitro compound - C-nitro compound - Secondary carboxylic acid amide - Carboxamide group - Carboxylic acid derivative - Organic oxoazanium - Allyl-type 1,3-dipolar organic compound - Propargyl-type 1,3-dipolar organic compound - Organic 1,3-dipolar compound - Azacycle - Organic nitrogen compound - Organonitrogen compound - Organooxygen compound - Organic zwitterion - Organic salt - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Aromatic heteropolycyclic compound |
| Beschreibung | This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds). |
| External Descriptors | Not available |
| Löslichkeit | Solubility (25°C) In vitro DMSO: 16 mg/mL (49.33 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| DMSO (mg/ml) Maximale Löslichkeit | 65 |
| DMSO (mM) Maximale Löslichkeit | 200.413159436377 |
| Wasser (mg/ml) Maximale Löslichkeit | ＜1 |
| Molekulargewicht | 324.330 g/mol |
| XLogP3 | 3.300 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Exact Mass | 324.122 Da |
| Monoisotopic Mass | 324.122 Da |
| Topological Polar Surface Area | 92.700 Ų |
| Heavy Atom Count | 24 |
| Formal Charge | 0 |
| Complexity | 467.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
