LMK-235

Catalog No.S7569 Batch:S756904

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Technical Data

Formula

C15H22N2O4
Molecular Weight 294.35 CAS No. 1418033-25-6
Solubility (25°C)* In vitro DMSO 7 mg/mL (23.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
Targets
HDAC5 [1]
(Cell-free assay)		 HDAC4 [1]
(Cell-free assay)
4.2 nM 11.9 nM
In vitro

LMK-235 causes HDAC inhibition with IC50 of <1 μM in human cancer cell lines with different sensitivity. 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. [1]

In addition, LMK-235 also shows nanomolar activity against multiple malaria parasite life cycle stages. [2]
In vivo

LMK-235 is a selective inhibitor of HDAC4.

Protocol (from reference)

Kinase Assay:

[1]
  • HDAC IC50 Profiling

    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 is used as reference compounds.
Cell Assay:

[1]
  • Cell lines

    A2780, Cal27, Kyse510, and MDA-MB-231 cell lines

  • Concentrations

    ~10 μM

  • Incubation Time

    72 hours

  • Method

    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.
Animal Study:

[3]
  • Animal Models

    C57BL/6-BALB/c mice

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Clin Epigenetics, 2018, 10(1):120]

Data from [Data independently produced by , , Oncotarget, 2016, 7(39):63829-63838]

Data from [Data independently produced by , , Oncotarget, 2016, 7(25):37966-37978]

Data from [Data independently produced by , , J Biol Chem, 2016, 291(14):7386-95.]

Selleck's LMK-235 has been cited by 40 publications

Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
Silica's silent threat: Contributing to skin fibrosis in systemic sclerosis by targeting the HDAC4/Smad2/3 pathway [ Environ Pollut, 2024, 355:124194] PubMed: 38782158
A COMPARATIVE ANALYSIS TO DETERMINE THE OPTIMUM HISTONE DEACETYLASE INHIBITORS AND ADMINISTRATION ROUTE FOR IMPROVING SURVIVAL AND ORGAN INJURY IN RATS AFTER HEMORRHAGIC SHOCK [ Shock, 2023, 60(1):75-83] PubMed: 37141162
Protective effect of HDACIs in improves survival and organ injury after CLP-induced sepsis [ Surg Open Sci, 2023, 12:35-42] PubMed: 36936452
Kinase signalling in excitatory neurons regulates sleep quantity and depth [ Nature, 2022, 612(7940):512-518] PubMed: 36477539
HDAC5-mediated Smad7 silencing through MEF2A is critical for fibroblast activation and hypertrophic scar formation [ Int J Biol Sci, 2022, 18(15):5724-5739] PubMed: 36263180
Yeast beta-glucan mediates histone deacetylase 5-induced angiogenesis in vascular endothelial cells [ Int J Biol Macromol, 2022, 211:556-567] PubMed: 35569678
Leveraging patient derived models of FGFR2 fusion positive intrahepatic cholangiocarcinoma to identify synergistic therapies [ NPJ Precis Oncol, 2022, 6(1):75] PubMed: 36274097
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147] PubMed: 36371227
HDAC5-Mediated Acetylation of p100 Suppresses Its Processing [ Int Dent J, 2022, S0020-6539(22)00199-X] PubMed: 36156247

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.