Droxinostat

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Chemical Structure| 99873-43-5 同义名 : NS 41080
CAS号 : 99873-43-5
货号 : A193904
分子式 : C11H14ClNO3
纯度 : 99%+
分子量 : 243.69
MDL号 : MFCD01326592
存储条件：

Pure form Inert atmosphere,2-8°C

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

DMSO: 145 mg/mL(595.02 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：

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

生物活性
靶点

  • HDAC8

    HDAC8, IC50:1.46 μM

  • HDAC3

    HDAC3, IC50:16.9 μM

  • HDAC6

    HDAC6, IC50:2.47 μM
描述 Droxinostat is a selective inhibitor of HDAC3, 6 and 8 with IC50 values of 16.9μM, 2.47μM and 1.46μM, respectively. Droxinostat inhibited HDAC activity and up-regulated ac-H3 in PPC-1, OVCAR-3, HT29, U937, and T47D cancer cells at 50μM post 16h. Inhibition of HDAC3, HDAC6, and HDAC8 by Droxinostat dose-dependently sensitized resistant PPC-1 prostate cancer cells to FAS at concentration ranging in 20-80μM, suggesting it may work as a chemical sensitizer to death receptor stimuli, decreasing the expression of the caspase-8 inhibitor FLIP[2].
作用机制 The hydroxamic acid of Droxinostat binds to the zinc ion in the active site of HDAC8.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.10mL

0.82mL

0.41mL

20.52mL

4.10mL

2.05mL

41.04mL

8.21mL

4.10mL
参考文献

[1]Wood TE, Dalili S, et al. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56.

[2]Wood TE, Dalili S, Simpson CD, Sukhai MA, Hurren R, Anyiwe K, Mao X, Suarez Saiz F, Gronda M, Eberhard Y, MacLean N, Ketela T, Reed JC, Moffat J, Minden MD, Batey RA, Schimmer AD. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56. doi: 10.1158/1535-7163.MCT-09-0495. Epub 2010 Jan 6. PMID: 20053768.