WT-161 是有效选择性的 HDAC6 抑制剂，IC₅₀ 值为 0.40 nM。WT-161 还抑制 MBLAC2。

WT-161 is a potent and selective HDAC6 inhibitor with an IC 50 of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2).

Solid

HDAC6 0.4 nM (IC50) HDAC1 8.35 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hideshima T, et al. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167.
[2]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28.

In Vitro: DMSO : ≥ 100 mg/mL (218.08 mM)配制储备液