| Bioactivity | WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM[1]. WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2)[2]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | WT-161 | ||||||||||||
| CAS | 1206731-57-8 | ||||||||||||
| Formula | C27H30N4O3 | ||||||||||||
| Molar Mass | 458.55 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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