10mM in DMSO para fluxos de trabalho cromatográficos e analíticos sensíveis que exigem interferência mínima da linha de base.
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Information
WT161 is a potent, selective, and bioavailableHDAC6inhibitor withIC50 valuesof 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 inducesapoptosis.
Targets
HDAC6 (Cell-free assay); HDAC1 (Cell-free assay); HDAC2 (Cell-free assay) 0.4 nM; 8.35 nM; 15.4 nM
In vitro
WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. It induces accumulation of acetylated tubulin and cytotoxicity in multiple myeloma (MM) cells. WT161 as a single agent does not induce ER stress, the UPR, or ER stress-mediated apoptosis. Consistent with WT-161 mediated hyperacetylation and inhibition of hsp90 chaperone function, treatment with WT-161 increases the intracellular levels of polyubiuitylated proteins in the cultured MCL JeKo-1 and Z138 cells. WT-161 also dose-dependently depletes the levels of cyclin D1 in the cultured human Mantle Cell Lymphoma (MCL) cells. Treatment with WT-161 induces ER stress response in the MCL cells, demonstrated by increase in the protein levels of Glucose regulated protein (GRP) 78, phosphorylated eIF2 (eukaryotic initation factor 2) α, and induction of the pro-apoptotic transcription factor CHOP (CAAT/Enhancer Binding Protein Homologous Protein). WT161 triggers apoptotic cell death in MCF7, T47D, BT474, and MDA-MB231 cells, associated with decreased expression of EGFR, HER2, and ERα and downstream signaling.
In vivo
WT161 has reasonable half-life in mice (1.4 h) and drug exposure [maximum concentration (Cmax) = 18 mg/L]. It is well tolerated as a single agent. WT161 significantly inhibits in vivo MCF7 cell growth, associated with downregulation of ERα, in a murine xenograft model.
Cell Research(from reference)
Cell lines：MM.1S cells\xa0
Concentrations：3 µM
Incubation Time：16 h
Documento abrangente sobre perigos, manuseamento, armazenamento e conformidade regulamentar.
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Consultar COA →Resumo de referência rápida das especificações e aplicações do produto.
Ver ficha técnica →Atributos de qualidade completos e critérios de aceitação para este grau.
Ver folha de especificações →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organic nitrogen compounds |
| Classe | Organonitrogen compounds |
| Subclass | Amines |
| Intermediate Tree Nodes | Tertiary amines |
| Direct Parent | Triarylamines |
| Alternative Parents | Aniline and substituted anilines Hydroxamic acids Amino acids and derivatives Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic homomonocyclic compounds |
| Substituents | Tertiary aromatic amine - Aniline or substituted anilines - Benzenoid - Monocyclic benzene moiety - Hydroxamic acid - Amino acid or derivatives - Carboxylic acid derivative - Organic oxygen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Carbonyl group - Aromatic homomonocyclic compound |
| Descrição | This compound belongs to the class of organic compounds known as triarylamines. These are organic compounds containing a trialkylamine group, characterized by exactly three aryl groups bonded to the amino nitrogen. |
| External Descriptors | Not available |
| DMSO (mg/mL) Solubilidade máxima | 86 |
|---|---|
| DMSO (mM) Solubilidade máxima | 187.5477047 |
| Água (mg/mL) Solubilidade máxima | ＜1 |
| Peso molecular | 458.600 g/mol |
| XLogP3 | 4.900 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 12 |
| Exact Mass | 458.232 Da |
| Monoisotopic Mass | 458.232 Da |
| Topological Polar Surface Area | 94.000 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 603.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 1 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 1 |
| Covalently-Bonded Unit Count | 1 |
