WT161 |
| Catalog No.GC18206 |
WT161은 IC50이 0.40nM인 강력하고 선택적인 HDAC6 억제제입니다. WT161은 또한 메탈로-β-락타마제 도메인 함유 단백질 2(MBLAC2)을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1206731-57-8
Sample solution is provided at 25 µL, 10mM.
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WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
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].
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].
References:
[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.
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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