Size | Price | Stock |
---|---|---|
5mg | $80 | In-stock |
10mg | $130 | In-stock |
25mg | $245 | In-stock |
50mg | $360 | In-stock |
100mg | $520 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-100871 |
M.Wt: | 458.55 |
Formula: | C27H30N4O3 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 100 mg/mL (218.08 mM) |
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]. IC50 & Target: IC50: 0.40 nM (HDAC6), 51.61 nM (HDAC3)[1] 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].
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