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TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs. TMP269 showes no effect at the acetylation level of histone H3-K9, no signifcant effects (2-fold) in gene expression on T-cells and no cytotoxicity in T cell expansion assay. TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation.In addition, TMP269 significantly promotes reprogramming.
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Source | Breast Cancer Res Treat (2014). Figure 1. TMP269 |
| Method | qPCR | |
| Cell Lines | MDAMB-231 cells | |
| Concentrations | 100 nM | |
| Incubation Time | 24 h | |
| Results | Quantitation of the CV assay dose response (10nM–10μM) in MDA-MB-231 cells demonstrated a similar effect on cell proliferation by LBH589 as previously observed, while SAHA and TMP269 were much less effective |
| Cell Experiment | |
|---|---|
| Cell lines | Human CD4+ T cells |
| Preparation method | Isolating human CD4+ T cells from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plating at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer’s instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells. |
| Concentrations | 10 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 514.52 |
| Formula | C25H21F3N4O3S |
| CAS Number | 1314890-29-3 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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