LMK-235

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Technical Data

Molecular Weight 294.35 Storage powder
Formula

C15H22N2O4

in solvent
CAS No. 1418033-25-6 Synonyms N/A
Solubility (25°C) * In vitro DMSO 58 mg/mL (197.04 mM)
Ethanol 58 mg/mL (197.04 mM)
Water Insoluble
In vivo
* <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.
Chemical Name N-(6-(hydroxyamino)-6-oxohexyloxy)-3,5-dimethylbenzamide

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

Protocol (Only for 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 and vorinostat are 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.

 

References

Customer Product Validation

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

Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.

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

MDA-MB-231 and Hs-578T cells were treated with DMSO or 50 nM, 500 nM, or 1 μM LMK-235 for 24 hours. The levels of acetyl-histone H3 and total histone H3 were examined by western blot. GAPDH was used as a loading control.

LMK-235 has been referenced in 3 publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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