化学性质:
规格 | 10mM (in 1mL DMSO) 10mg 50mg |
CAS | 1418033-25-6 |
别名 |
|
化学名 | N-((6-(hydroxyamino)-6-oxohexyl)oxy)-3,5-dimethylbenzamide |
分子式 | C15H22N2O4 |
分子量 | 294.35 |
溶解度 | ≥ 9.95mg/mL in DMSO, ≥ 53.8 mg/mL in EtOH with ultrasonic |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
Description:
IC50: cytotoxicity IC50 (490 nm for A2780; 320 nm for A2780 CisR); HDAC inhibition (650 nM for A2780; 320 nm for A2780 CisR)
Histone deacetylases (EC
In vitro: LMK235 showed similar effects compared to vorinostat on inhibition of cellular HDACs in a pan-HDAC assay but enhanced cytotoxic effects against the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231. LMK235 shows nanomolar inhibition of HDAC4 and HDAC5, whereas vorinostat and TSA inhibit HDAC4 and HDAC5 in the higher micromolar range. In contrast to vorinostat, LMK235 showed a novel HDAC isoform selectivity profile with preference for HDAC4 and HDAC5, which are inhibited with low nanomolar IC50 values [1].
In vivo: In a mouse in-vivo study, synergistic inhibition was demonstrated for LMK235 and Cytarabine in proliferation assays and in colony formation assays. These findings demonstrate that in vivo RNAi screening for therapeutic efficacy is feasible. HDAC4 might be an important target to enhance efficacy of anti-leukemic drugs [2].
Clinical trial: LMK235 is currently in the preclinical development and no clinical trial is ongoing.
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