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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
TH34 is aHDACinhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM).
Targets
HDAC8 ; HDAC6 ; HDAC10 1.9 μM; 4.6 μM; 7.7 μM
In vitro
TH34 strongly binds to HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM), and shows no substantial affinity to HDAC2 at concentrations up to 50 µM. Its treatment induces hyperacetylation of tubulin and SMC3. TH34 effectively and selectively eliminates high-grade neuroblastoma cells while sparing non-transformed human cells. In neuroblastoma cell lines as well as primary neuroblastoma cells, it markedly induces DNA damage, followed by differentiation and G2/M phase cell cycle arrest at later timepoints, eventually leading to cell death.
Cell Research(from reference)
Cell lines：SK-N-BE(2)-C cells
Concentrations：10 μM
Incubation Time：48 h
Umfassendes Dokument zu Gefahren, Handhabung, Lagerung und Einhaltung regulatorischer Vorschriften.
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Spezifikationsblatt ansehen →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Klasse | Benzene and substituted derivatives |
| Subclass | Phenylmethylamines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylbenzamines |
| Alternative Parents | Aminobenzoic acids and derivatives p-Toluamides Phenylalkylamines Benzylamines Benzoyl derivatives Aniline and substituted anilines Aminotoluenes Secondary alkylarylamines Hydroxamic acids Amino acids and derivatives Organopnictogen compounds Organooxygen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic homomonocyclic compounds |
| Substituents | Phenylbenzamine - Aminobenzoic acid or derivatives - P-toluamide - Toluamide - Benzoic acid or derivatives - Aminotoluene - Phenylalkylamine - Aniline or substituted anilines - Benzylamine - Benzoyl - Aralkylamine - Toluene - Secondary aliphatic/aromatic amine - Hydroxamic acid - Amino acid or derivatives - Secondary amine - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Amine - Aromatic homomonocyclic compound |
| Beschreibung | This compound belongs to the class of organic compounds known as phenylbenzamines. These are aromatic compounds consisting of a benzyl group that is N-linked to a benzamine. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Löslichkeit | Solubility (25°C) In vitro DMSO: 51 mg/mL (198.98 mM); Ethanol: 15 mg/mL (58.52 mM); Water: Insoluble; |
|---|---|
| Empfindlichkeit | light sensitive |
| DMSO (mg/ml) Maximale Löslichkeit | 51 |
| DMSO (mM) Maximale Löslichkeit | 198.985563792431 |
| Wasser (mg/ml) Maximale Löslichkeit | ＜1 |
| Molekulargewicht | 256.300 g/mol |
| XLogP3 | 2.600 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 4 |
| Exact Mass | 256.121 Da |
| Monoisotopic Mass | 256.121 Da |
| Topological Polar Surface Area | 61.400 Ų |
| Heavy Atom Count | 19 |
| Formal Charge | 0 |
| Complexity | 290.000 |
| 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 |
F2220439