MS-275 (Entinostat) is a potent Histone Deacetylase inhibitor with IC50 value of 0.3 and 8µM for HDAC1 and HDAC3 respectively. It 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.
|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 (Dojindo), and absorbance was quantified after 2 h using a SpectraMax microplate reader (Molecular Devices). 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 (Xenogen) using a 15-s exposure. Luminescence was quantified using Living Image software (Xenogen). For both assays, cell survival was expressed as a percentage of vehicle-treated control values.|
|Incubation time||24, 48, or 72 h|
|Animal models||LHβ-Tag mice model|
|Dosages||every other day for 21 d with 20 mg/kg MS-275|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Histone deacetylase inhibitors suppress mechanical stress-induced expression of RUNX-2 and ADAMTS-5 through the inhibition of the MAPK signaling pathway in cultured human chondrocytes.
Saito T, et al. Osteoarthritis Cartilage. 2012 Sep 24. PMID: 23017871.
MS-275 sensitizes osteosarcoma cells to Fas ligand-induced cell death by increasing the localization of Fas in membrane lipid rafts.
Rao-Bindal K, et al. Cell Death Dis. 2012 Aug 9;3:e369. PMID: 22875006.
MS-275, a benzamide histone deacetylase inhibitor, prevents osteoclastogenesis by down-regulating c-Fos expression and suppresses bone loss in mice.
Kim HN, et al. Eur J Pharmacol. 2012 Sep 15;691(1-3):69-76. PMID: 22846626.
P38 MAP kinase functions as a switch in MS-275-induced reactive oxygen species-dependent autophagy and apoptosis in human colon cancer cells.
Zhan Y, et al. Free Radic Biol Med. 2012 Aug 1;53(3):532-43. PMID: 22634147.
Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma.
Dalgard CL, et al. Clin Cancer Res. 2008 May 15;14(10):3113-23. PMID: 18483379.
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