1206731-57-8
1206731-57-8 structure
- Name: WT-161
- Chemical Name: WT-161
- CAS Number: 1206731-57-8
- Molecular Formula: C27H30N4O3
- Molecular Weight: 458.552
- Catalog: Research Areas Cancer
- Create Date: 2018-03-16 03:22:59
- Modify Date: 2024-02-28 09:03:04
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WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
| Name | WT-161 |
|---|---|
| Synonyms |
Octanoic acid, 8-(hydroxyamino)-8-oxo-, 2-[(1E)-[4-(diphenylamino)phenyl]methylene]hydrazide
8-{(2E)-2-[4-(Diphenylamino)benzylidene]hydrazino}-N-hydroxy-8-oxooctanamide |
| Description | WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM. |
|---|---|
| Related Catalog | |
| Target |
HDAC6:0.4 nM (IC50) HDAC1:8.35 nM (IC50) HDAC2:15.4 nM (IC50) HDAC3:51.6 nM (IC50) HDAC8:1430 nM (IC50) |
| In Vitro | WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 µM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance[1]. |
| In Vivo | WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect[1]. |
| Cell Assay | MM.1S cells are treated with increasing concentrations of WT161 (0-10 μM) for 48 hours. Cell viability is determined using the MTT assay[1]. |
| Animal Admin | Mice: Mice tumor xenograft are assigned into cohorts receiving vehicle (control), BTZ (0.5 mg/kg, i.v.), WT161 (50 mg/kg, i.p.), or BTZ+WT161. WT161 is administered for five consecutive days each week, and BTZ is given on a twice-weekly schedule. Caliper measurements of the longest perpendicular tumor diameters are performed on alternate days to estimate the tumor volume[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Molecular Formula | C27H30N4O3 |
| Molecular Weight | 458.552 |
| Exact Mass | 458.231781 |
| LogP | 5.34 |
| Index of Refraction | 1.594 |
| Storage condition | -20℃ |