WT-161

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Chemical Structure| 1206731-57-8 同义名 : -
CAS号 : 1206731-57-8
货号 : A756883
分子式 : C27H30N4O3
纯度 : 99%+
分子量 : 458.552
MDL号 : MFCD31563598
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(228.98 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HDAC6

    HDAC6, IC50:0.4 nM

  • HDAC2

    HDAC2, IC50:15.4 nM

  • HDAC1

    HDAC1, IC50:8.35 nM
描述 WT161 is a selective and potent HDAC6 inhibitor with IC50 value of 0.6nM, much potent to HDAC6 than HDAC1 (IC50=8.35nM) and HDAC2 (IC50=15.4nM). Inhibition of HDAC6 through WT161 at concentration ranging in 0.3-3μM dose-dependently up-regulated acetylation of tubulin in MM.1S cells post 6h. WT161 in combination with bortezomib triggered significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. And this combined treatment of WT161 (50mg/kg, i.p.) and bortezomib (0.5mg/kg, i.v.) for 26 days also inhibited tumor growth in SCID mice injected s.c. with MM.1S cells[3].
作用机制 WT161 can interact with active site pocket of HDAC2, HDAC3, and HDAC6. It chelate the zinc ion through the hydroxamic acid.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.90mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL
参考文献

[1]Hideshima T, Qi J, 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. Epub 2016 Oct 31.

[2]Hideshima T, Mazitschek R, et al. HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer. Oncotarget. 2017 Jul 5;8(46):80109-80123.

[3]Hideshima T, Qi J, Paranal RM, Tang W, Greenberg E, West N, Colling ME, Estiu G, Mazitschek R, Perry JA, Ohguchi H, Cottini F, Mimura N, Görgün G, Tai YT, Richardson PG, Carrasco RD, Wiest O, Schreiber SL, Anderson KC, Bradner JE. 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. doi: 10.1073/pnas.1608067113. Epub 2016 Oct 31. PMID: 27799547; PMCID: PMC5135369.