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    LMK-235
    LMK-235

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    产品仅用于科学研究,不针对患者销售
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    InvivoChem目录号 #: V0266
    CAS号码 #: 1418033-25-6纯度 ≥98%

    Description: LMK-235 is a novel, potent and selective inhibitor of HDAC4 and HDAC5 (histone deacetylase) with potential antitumor activity. It inhibits HDAC4/5 with IC50s of 11.9 nM and 4.2 nM, respectively. It has IC50s of 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM for HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, respectively. LMK235 showed similar effects compared to vorinostat on inhibition of cellular HDACs in a pan-HDAC assay but enhanced cytotoxic effects against the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231. LMK235 shows nanomolar inhibition of HDAC4 and HDAC5, whereas vorinostat and TSA inhibit HDAC4 and HDAC5 in the higher micromolar range. In contrast to vorinostat, LMK235 showed a novel HDAC isoform selectivity profile with preference for HDAC4 and HDAC5, which are inhibited with low nanomolar IC50 values. 

    ReferencesJ Med Chem. 2013 Jan 24;56(2):427-36; Eur J Med Chem. 2014 Jul 23;82:204-13. 

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    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 


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LMK-235
    J Med Chem. 2013 Jan 24;56(2):427-36.

    LMK-235

    Hyperacetylation of P. falciparum histones. (Compound 1a is LMK-235) Eur J Med Chem. 2014 Jul 23;82:204-13.

    LMK-235

    LMK-235 synergizes with bortezomib in BC cells.  2016 Jun 21;7(25):37966-37978.

     

    LMK-235

    LMK-235 inhibits BC cell proliferation and induces apoptosis.  2016 Jun 21;7(25):37966-37978.


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