LMK-235

Catalog No.S7569

LMK-235 Chemical Structure

Molecular Weight(MW): 294.35

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

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3 Customer Reviews

  • 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.

    Oncotarget, 2016, 7(39):63829-63838. LMK-235 purchased from Selleck.

    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.

    Oncotarget, 2016, 7(25):37966-37978. LMK-235 purchased from Selleck.

  • B, 5×106 293T, HeLa, A549, and H1299 cells were seeded in 10-cm dishes on day 0 and treated with dimethyl sulfoxide, 10 μM TMP269, 10 μM LMK-235, or butyrate as indicated for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and β-actin. D, 1×106 293T cells were plated in 10-cm dishes on day 0 and transfected with 2 μg of vector plasmids or plasmids encoding FLAG-HDAC1 as indicated on day 1. On day 3, the cells were treated with butyrate sodium solution for 12 h. Cell lysates were collected and subjected to Western blotting analysis of Apaf-1, HDAC1, FLAG, and GAPDH.

    J Biol Chem, 2016, 291(14):7386-95.. LMK-235 purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2780 cells MX;DfZRwfG:6aXPpeJkh[XO|YYm= NGntcYY4OiCq MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBkcXOybHH0bY4hemW|aYP0ZY51KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{OiEQvF2= NXrYXnhTOjN{NUK2NFM>
human A2780 cells MX7DfZRwfG:6aXPpeJkh[XO|YYm= NGrKO4Y4OiCq MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuOFkh|ryP MmDnNlMzPTJ4MEO=
human A2780 cells NVfBflB4S3m2b4TvfIlkcXS7IHHzd4F6 M4XZfFE5KGh? MU\Jcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgNVghcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4Phfg+9lCCLQ{WwQVAvPjVizszN NITuWYIzOzJ3Mk[wNy=>
human HepG2 cells NWr5SmwzS3m2b4TvfIlkcXS7IHHzd4F6 Mn\XOFghcA>? MkfUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgOFghcHK|LDDJR|YxRTFwMk[g{txO NGPOVJkzPDlyNEm2Oy=>
human MDA-MB-231 cells NETlfGtEgXSxdH;4bYNqfHliYYPzZZk> MlPSO|IhcA>? MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBkcXOybHH0bY4he2Wwc3n0bZZmKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkO3JO69VQ>? MY[yN|I2OjZyMx?=
human KYSE-510 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= MVy3NkBp NGXSU3pEgXSxdH;4bYNqfHliYXfhbY5{fCClaYPwcIF1cW5icnXzbZN1[W62IHj1cYFvKEu\U1WtOVExKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj60PEDPxE1? MomzNlMzPTJ4MEO=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

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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 Research:

[1]

+ Expand
  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (197.04 mM)
Ethanol 58 mg/mL (197.04 mM)
Water 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 Information

Molecular Weight 294.35
Formula

C15H22N2O4

CAS No. 1418033-25-6
Storage powder
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID