LMK-235 Chemical Properties

Melting point:

135-138°C

Density 

1.155±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

9.46±0.20(Predicted)

color 

white to beige

InChIKey

VRYZCEONIWEUAV-UHFFFAOYSA-N

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

3

LMK-235 Usage And Synthesis

Description

Histone deacetylases (HDACs) catalyze the hydrolytic removal of acetyl groups from histone lysine residues, which commonly results in chromatin condensation and transcriptional repression. LMK 235 is an HDAC inhibitor that selectively targets HDACs 4 and 5 (IC₅₀s = 12 and 4 nM, respectively) over other HDACs (IC₅₀s = 56, 320, 850, 880, and 1,280 for HDACs 6, 1, 11, 2, and 8, respectively). It displays enhanced cytotoxic effects against human cancer cell lines, compared to SAHA or trichostatin A . LMK 235 and derivatives inhibit the growth of the malarial parasite P. falciparum at multiple life cycle stages at nanomolar concentrations.

Uses

LMK 235 is a histone deacetylase (HDAC)4 and HDAC5 inhibitor and has shown to have enhanced cytotoxic effects against the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231.

Biochem/physiol Actions

LMK-235 induces the differentiation of odontoblasts in dental pulp cells. It plays an important role in the regeneration of dental tissue.

in vivo

IC 50

HDAC5: 4.22 nM (IC₅₀); HDAC4: 11.9 nM (IC₅₀); HDAC6: 55.7 nM (IC₅₀); HDAC1: 320 nM (IC₅₀); HDAC11: 852 nM (IC₅₀); HDAC2: 881 nM (IC₅₀); HDAC8: 1278 nM (IC₅₀)

References

[1] BRIAN D. STRAHL  C. D A. The language of covalent histone modifications[J]. Nature, 2000, 403 6765: 41-45. DOI: 10.1038/47412
[2] WANG L CHEUNG  C D A  Scott D Briggs. Acetylation and chromosomal functions[J]. Current Opinion in Cell Biology, 2000, 12 3: Pages 326-333. DOI: 10.1016/s0955-0674(00)00096-x
[3] LINDA MAREK. Histone Deacetylase (HDAC) Inhibitors with a Novel Connecting Unit Linker Region Reveal a Selectivity Profile for HDAC4 and HDAC5 with Improved Activity against Chemoresistant Cancer Cells[J]. Journal of Medicinal Chemistry, 2012, 56 2: 427-436. DOI: 10.1021/jm301254q
[4] FINN K. HANSEN . Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages[J]. European Journal of Medicinal Chemistry, 2014, 82: Pages 204-213. DOI: 10.1016/j.ejmech.2014.05.050

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