LMK235 is a potent and selective histone deacetylase HDAC4 and HDAC5 inhibitor (IC50 ~11.9 nM and 4.22 nM respectively). It also has inhibitory activities against HDAC 6, 1, 11, 2, and 8 with IC50 for 55.7, 320, 852, 881, and 1278 nM, respectively. LMK235 exhibits cytotoxity against chemo-resistant cancer cell lines in human ovarian cancer cell lines A2780 and cisplatin resistant A2780CisR (IC50 ~0.49 and 0.32 μM respectively).
CAS Number: 1418033-25-6
Molecular Weight: 294.35
Chemical Name: N-((6-(hydroxyamino)-6-oxohexyl)oxy)-3,5-dimethylbenzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
LMK235 shows cytotoxic activity against human ovarian cancer cell lines A2780 and A2780 CisR, with IC50s of 0.49 μM and 0.32 μM, respectively. LMK-235 inhibits HDAC in A2780 and A2780 CisR cell lines, with IC50s of 0.65 μM and 0.32 μM, respectively. LMK-235 produces a higher reduction in cell viability in comparison to the combination of cisplatin and vorinostat in all cell lines. LMK-235 (0, 0.625, 1.25, 2.5, 5, 10, and 20 μM) reduces the proliferation of BC cells in a dose- and time-dependent manner. LMK-235 (0-800 nM) also inhibits the growth of BC cells. Moreover, LMK-235 synergizes with bortezomib in BC cell lines. LMK235 (2, 20 nM) decreases in HDAC4 nuclear accumulation in Cdkl5 -/Y NPCs, completely restores the reduced number of neurons generated from Cdkl5 -/Y NPCs. LMK235 also restores histone 3 acetylation in Cdkl5 -/Y NPCs. LMK235 causes a notable increase in the isoform IV, but does not affect BDNF isoforms I or II.
LMK235 (5 and 20 mg/kg) restores survival and maturation of postmitotic granule neurons in Cdkl5 -/Y mice. LMK235 also restores synapse development in the dentate gyrus and hippocampus of Cdkl5 -/Y mice. Furthermore, LMK235 restores hippocampus-dependent learning and memory in Cdkl5 -/Y mice.
- Hansen FK, Sumanadasa SD, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, MordmÃ¼ller B, Kassack MU, Winzeler EA, Avery VM, Andrews KT, Kurz T. Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. Eur J Med Chem. 2014 Jul 23;82:204-13. doi: 10.1016/j.ejmech.2014.05.050. Epub 2014 May 22. PubMed PMID: 24904967.
- Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. 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. 2013 Jan 24;56(2):427-36. doi: 10.1021/jm301254q. Epub 2013 Jan 8. PubMed PMID: 23252603.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.