1206731-57-8
WT-161
CAS: 1206731-57-8
Molecular Formula: C27H30N4O3
1206731-57-8 - Names and Identifiers
| Name | WT-161 |
| Synonyms | WT161 WT-161 CS-2547 WT 161 WT-III-161 Octanoic acid, 8-(hydroxyamino)-8-oxo-, 2-[[4-(diphenylamino)phenyl]methylene]hydrazide |
| CAS | 1206731-57-8 |
1206731-57-8 - Physico-chemical Properties
| Molecular Formula | C27H30N4O3 |
| Molar Mass | 458.55 |
| Density | 1.15±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 100 mg/mL |
| pKa | 9.48±0.20(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | WT161 selectively inhibited HDAC6 and significantly increased the level of acetylated α-tubulin, with little effect on overall lysine acetylation. It is able to induce the accumulation and toxicity of acetylated tubulin in multiple myeloma cells. WT161 monotherapy did not induce ER stress response, UPR or ER stress-related apoptosis. In cultured MCL JeKo-1 and Z138 cells, WT-161 treatment will increase intracellular ubiquitinated protein levels. In cultured MCL cells (mantle cell lymphoma), WT-161 dose-dependently depletes cyclin D1 levels. WT-161 treatment can also induce ER stress response in MCL cells -- the increase of GRP78 protein level and phosphorylated eIF2α level, and the induction of pro-apoptotic transcription factor CHOP. WT161 can cause apoptotic cell death of MCF7, T47D, BT474 and MDA-MB231 cells, and decrease the expression of EGFR, HER2, ERα and downstream signals. |
| In vivo study | WT161 has a reasonable Half-Life (1.4 H) and drug exposure (Cmax = 18 mg/L) in mice. When treated with single drug administration, it was well tolerated. WT161 can significantly inhibit the growth of MCF7 cells in vivo and down-regulate the expression of ERα in a xenograft tumor mouse model. |
1206731-57-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.181 ml | 10.904 ml | 21.808 ml |
| 5 mM | 0.436 ml | 2.181 ml | 4.362 ml |
| 10 mM | 0.218 ml | 1.09 ml | 2.181 ml |
| 5 mM | 0.044 ml | 0.218 ml | 0.436 ml |
Last Update：2024-01-02 23:10:35
1206731-57-8 - Reference Information
| biological activity | WT161 is a potent, selective inhibitor of HDAC6, the IC50 values of HDAC1 and HDAC2 were 0.4 nM, 8.35 nM and 15.4 nM, respectively, which was more than 100 times higher than that of other HDACs. WT161 can induce apoptosis. |
| Target | Value |
| HDAC6 (Cell-free assay) | 0.4 nM |
| HDAC1 (Cell-free assay) | 8.35 nM |
| HDAC2 (Cell-free assay) | 15.4 nM |
Last Update：2024-04-09 21:01:54
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Product Name: WT-161 Visit Supplier Webpage Request for quotation
CAS: 1206731-57-8
Tel: 18301782025
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Mobile: 18021002903
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CAS: 1206731-57-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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