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CAS No.: 1418033-25-6

LMK-235 Catalog No. CSN17824

Synonyms: LMK-235

LMK235 is a HDAC inhibitor of human HDAC4 and HDAC5 with IC50 values of 0.49 μM (A2780) and 0.32 μM (A2780 CisR).

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC5

IC50:0.32μM HDAC4

IC50:0.49μM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 1 mg/kg, 3 mg/kg^[2] (i.p.), 5 mg/kg - 30 mg/kg^[3] (right lateral ventricle through a 25 μl Hamilton syringe)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 1 mg/kg, 3 mg/kg^[2] (i.p.), 5 mg/kg - 30 mg/kg^[3] (right lateral ventricle through a 25 μl Hamilton syringe)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3974 mL
- 16.9868 mL
- 33.9736 mL
- 5 mM
- 0.6795 mL
- 3.3974 mL
- 6.7947 mL
- 10 mM
- 0.3397 mL
- 1.6987 mL
- 3.3974 mL

技术信息

CAS号

1418033-25-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H22N2O4

运输

蓝冰

分子量

294.35

别名

LMK-235

溶解度

DMSO	58.0 mg/mL (197.0 mM)
Water	Insoluble
Ethanol	58.0 mg/mL (197.0 mM)

动物实验配方

5%DMSO+30%PEG300+5%TW80+water

13 mg/mL

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