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LMK-235
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LMK-235图片
CAS NO:1418033-25-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)294.35
FormulaC15H22N2O4
CAS No.1418033-25-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 58 mg/mL (197.0 mM)
Water: <1 mg/mL
Ethanol: 58 mg/mL (197.0 mM)
SMILES O=C(NOCCCCCC(NO)=O)C1=CC(C)=CC(C)=C1
Synonyms

LMK 235; LMK235; LMK-235

Chemical Name: N-((6-(hydroxyamino)-6-oxohexyl)oxy)-3,5-dimethylbenzamide

SMILES Code: O=C(NOCCCCCC(NO)=O)C1=CC(C)=CC(C)=C1

Exact Mass: 294.15796

实验参考方法
In Vitro

In vitro activity: LMK-235 causes HDAC inhibition with IC50 of<1 μM in human cancer cell lines with different sensitivity towards cisplatin. In breast cancer cell line MDA-MB-231, tongue cancer cell line Cal27, and esophagus cell line Kyse510 cell line, LMK-235 displays a high cytotoxicity, and markedly enhances the cytotoxicity of cisplatin. In addition, LMK-235 also shows nanomolar activity against multiple malaria parasite life cycle stages.


Kinase Assay: The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company’s standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds.


Cell Assay: The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow MTT to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance s measured at 544 and 690 nm in a FLUOstar microplate reader.

In VivoIn a mouse in-vivo study, synergistic inhibition was demonstrated for LMK235 and Cytarabine in proliferation assays and in colony formation assays. These findings demonstrate that in vivo RNAi screening for therapeutic efficacy is feasible. HDAC4 might be an important target to enhance efficacy of anti-leukemic drugs.
Animal modelMice
Formulation & Dosage5 and 20 mg/kg
References J Med Chem. 2013 Jan 24;56(2):427-36; Eur J Med Chem. 2014 Jul 23;82:204-13.