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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. 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.
Sci Rep. 2025 Nov 19;15:40178.
Selective HDAC6 inhibitor WT161 modulates the VLA-4/FAK pathway by inhibiting PKA activity in acute lymphoblastic leukemia.
WT161 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | MM cells |
| Preparation method | Cells cultured with WT161, BTZ, and CFZ were harvested, washed, and lysed using lysis buffer, and complete protease inhibitor mixture. |
| Concentrations | 1 µM |
| Incubation time | 6 h |
| Animal Experiment | |
|---|---|
| Animal models | mice |
| Formulation | |
| Dosages | 50–100 mg/kg |
| Administration | i.p. |
| Molecular Weight | 458.55 |
| Formula | C27H30N4O3 |
| CAS Number | 1206731-57-8 |
| Solubility (25°C) | 90 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Niltubacin
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| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
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