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Entinostat (MS-275) is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively. Entinostat inhibited in vitro cell growth in all cell lines tested with an IC50 ranging from 50 nM to 1.3 uM. MS-275 showed antiproliferative activity against all human breast cancer cell lines examined and induced TbRII mRNA, but not TGF-b type I receptor mRNA. MS-275 caused an accumulation of acetylated histones H3 and H4 in total cellular chromatin. An increase in the accumulation of acetylated histones H3 and H4 was detected in the TbRII promoter after treatment with MS-275.
Entinostat (MS-275) at 49 mg/kg shows marked antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and a moderate effect against Capan-1 tumor. Entinostat at 24.5 mg/kg and 12.3 mg/kg also shows significant effects against these tumors. In addition, oral administration of Entinostat apparently increases the level of histone acetylation in HT-29 tumor xenografts 4-24 h after the administration.
Front Neurosci. 2021 Apr 28;15:641284.
Valproic Acid Induces Autism-Like Synaptic and Behavioral Deficits by Disrupting Histone Acetylation of Prefrontal Cortex ALDH1A1 in Rats
Entinostat (MS-275) purchased from AbMole
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Source | Int J Clin Exp Pathol (2015). Figure 2. MS-275 |
| Method | i.v. | |
| Cell Lines | Sprague-Dawley rats | |
| Concentrations | 12.3, 24.5, 49.0 mg/kg | |
| Incubation Time | 7 days | |
| Results | There was no hepatocytic macrovesicular steatosis, lobular inflammatory cell infiltration and necrosis in both control group and MS-275 group |
| Cell Experiment | |
|---|---|
| Cell lines | HDACi-treated Y79, Weri-Rb1, and Y79-LUC human RB cell lines |
| Preparation method | Cell survival assays. For colorimetric analysis, cells were exposed to WST-8 Cell Proliferation Reagent, and absorbance was quantified after 2 h using a SpectraMax microplate reader. For bioluminescence analysis (Y79-LUC cells only), cells were exposed to 150 μg/mL D-luciferin, and plates were imaged in an IVIS Imaging System using a 15-s exposure. Luminescence was quantified using Living Image software. For both assays, cell survival was expressed as a percentage of vehicle-treated control values. |
| Concentrations | 0~100 μM |
| Incubation time | 24, 48, or 72 h |
| Animal Experiment | |
|---|---|
| Animal models | LHβ-Tag mice model |
| Formulation | DMSO |
| Dosages | every other day for 21 d with 20 mg/kg MS-275 |
| Administration | i.p. |
| Molecular Weight | 376.4 |
| Formula | C21H20N4O3 |
| CAS Number | 209783-80-2 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage | -20°C, sealed |
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| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
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