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.
|Source||Breast Cancer Res Treat (2014). Figure 1. TMP269|
|Cell Lines||MDAMB-231 cells|
|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 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.|
|Incubation time||72 hours|
|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.
Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling.
Sinnett-Smith J, et al. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71. PMID: 24647541.
Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.
Lobera M, et al. Nat Chem Biol. 2013 May;9(5):319-25. PMID: 23524983.
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