Home DNA Damage/DNA Repair HDAC inhibitor LMK-235 For research use only.

LMK-235

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

LMK-235 Chemical Structure

LMK-235 Chemical Structure

CAS No. 1418033-25-6

Purity & Quality Control

LMK-235 Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of p62 degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 23252603
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NCOA4 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 23252603
A2780 Function assay 18 hrs Inhibition of HDAC in resistant human A2780 cells after 18 hrs by fluorescence assay, IC50=0.32μM 23252603
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against resistant human A2780 cells after 72 hrs by MTT assay, IC50=0.32μM 23252603
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NBR1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 23252603
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NDP52 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 23252603
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of FTH1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 23252603
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=0.49μM 23252603
A2780 Function assay 18 hrs Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay, IC50=0.65μM 23252603
KYSE-510 Function assay 18 hrs Inhibition of HDAC in sensitive human KYSE-510 cells after 18 hrs by fluorescence assay, IC50=1μM 23252603
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against sensitive human CAL27 cells after 72 hrs by MTT assay, IC50=1.03μM 23252603
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against sensitive human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=1.37μM 23252603
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against resistant human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=1.68μM 23252603
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against resistant human CAL27 cells after 72 hrs by MTT assay, IC50=1.81μM 23252603
KYSE-510 Cytotoxicity assay 72 hrs Cytotoxicity against resistant human KYSE-510 cells after 72 hrs by MTT assay, IC50=2.48μM 23252603
KYSE-510 Cytotoxicity assay 72 hrs Cytotoxicity against sensitive human KYSE-510 cells after 72 hrs by MTT assay, IC50=2.96μM 23252603
HepG2 Antimalarial assay 48 hrs Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs, IC50=0.16μM 24904967
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs, IC50=1.26μM 24904967
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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 Research 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.
In Vivo
In vivo

LMK-235 is a selective inhibitor of HDAC4.
Animal Research Animal Models C57BL/6-BALB/c mice
Dosages 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 294.35 Formula

C15H22N2O4
CAS No. 1418033-25-6 SDF Download LMK-235 SDF
Smiles CC1=CC(=CC(=C1)C(=O)NOCCCCCC(=O)NO)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (200.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble


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In vivo
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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

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