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LMK-235

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Chemical Structure| 1418033-25-6 同义名 : -
CAS号 : 1418033-25-6
货号 : A135784
分子式 : C15H22N2O4
纯度 : 99%+
分子量 : 294.346
MDL号 : MFCD26522892
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(101.92 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：

5%DMSO+30%PEG300+5%TW80+water 13 mg/mL

生物活性
靶点

  • HDAC4

    HDAC4, IC50:11.9 nM

  • HDAC5

    HDAC5, IC50:4.2 nM
描述 LMK235 a potent hydroxamate-based HDAC inhibitor with IC50 values of 320, 881, 11.9, 4.22, 55.7, 1278 and 852nM for HDAC1, 2, 4, 5, 6, 8 and 11, respectively. LMK235 inhibited HDAC activity of sensitive/Cisplatin-resistent MDA-MB-231, Cal27 and Kyse510 cells with IC50 values of 0.46μM/0.41μM, 0.36μM/0.36μM and 1μM /0.35μM, respectively, and exhibited cell growth inhibitory effect on sensitive/Cisplatin-resistent MDA-MB-231, Cal27 and Kyse510 cells with IC50 values of 1.37μM/1.68μM, 1.03μM/1.81μM and 2.96μM and 2.48μM, respectively. Compared with vorinostat, LMK235 showed similar effects on inhibition of cellular HDACs, but enhanced cytotoxic effects against the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231. LMK-235 also showed nanomolar inhibition of HDAC4 and HDAC5, whereas vorinostat and TSA inhibit HDAC4 and HDAC5 in the higher micromolar range[2].
作用机制 LMK235 is a hydroxamate-based HDAC inhibitor which can chelate the catalytic zinc ion of HDAC. The alkoxyamide connecting unit linker region contributes to the selectivity of it.[2]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A2780 cells Cytotoxicity assay 72 h Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay, IC50=0.32 μM 23252603
human A2780 cells Cytotoxicity assay 72 h Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=0.49 μM 23252603
human A2780 cells Cytotoxicity assay 18 h Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay， IC50=0.65 μM 23252603
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

16.99mL

3.40mL

1.70mL

33.97mL

6.79mL

3.40mL
参考文献

[1]Marek L, Hamacher A, et al. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013 Jan 24;56(2):427-36.

[2]Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013 Jan 24;56(2):427-36. doi: 10.1021/jm301254q. Epub 2013 Jan 8. PMID: 23252603.