A selective inhibitor of HDAC4 and HDAC5
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LMK 235

Item No. 14969

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[6-(hydroxyamino)-6-oxohexyl]oxy]-3,5-dimethyl-benzamide
CAS Number
1418033-25-6
Molecular Formula
C15H22N2O4
Formula Weight
294.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
SMILES
CC1=CC(C)=CC(C(NOCCCCCC(NO)=O)=O)=C1
InChi Code
InChI=1S/C15H22N2O4/c1-11-8-12(2)10-13(9-11)15(19)17-21-7-5-3-4-6-14(18)16-20/h8-10,20H,3-7H2,1-2H3,(H,16,18)(H,17,19)
InChi Key
VRYZCEONIWEUAV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $80

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    10 mg

    $140

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    25 mg

    $293

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    Product Description

    Histone deacetylases (HDACs) catalyze the hydrolytic removal of acetyl groups from histone lysine residues, which commonly results in chromatin condensation and transcriptional repression.1,2 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).3 It displays enhanced cytotoxic effects against human cancer cell lines, compared to SAHA (Item No. 10009929) or trichostatin A (Item No. 89730).3 LMK 235 and derivatives inhibit the growth of the malarial parasite P. falciparum at multiple life cycle stages at nanomolar concentrations.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Strahl, B.D., and Allis, D. The language of covalent histone modifications. Nature 403(6765), 41-45 (2000).

    2. Cheung, W.L., Briggs, D.B., and Allis, C.D. Acetylation and chromosomal functions. Curr. Opin. Cell Biol. 12(3), 326-333 (2000).

    3. Marek, L., Hamacher, A., Hansen, F.K., et al. 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. Med. Chem. 56(2), 427-436 (2016).

    4. Hansen, F.K., Sumanadasa, S.D.M., Stenzel, K., et al. Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. Eur. J. Med. Chem. 82, 204-213 (2014).