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TMP269 is a highly potent and selective class IIa HDAC inhibitor identified, with IC50s of 126 nM, 80 nM, 36 nM and 19 nM for HDAC4, HDAC5, HDAC7 and HDAC9 respectively. TMP269 has an unprecedented metal-binding group, trifluoromethyloxadiazole (TFMO). The co-crystal structure of TMP 269 and HDAC7 revealed that bulky TFMO and U-shaped confirmation conferred potent and selective class IIa HDAC inhibition. 
In contrary to other HDAC inhibitors (TSA or SAHA), TMP269 showed 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.  However, inhibition of class IIa HDACs affected gene expression of CD14+ monocytes under PHA stimulation. This indicates the unique cellular activities of class IIa HDACs. The discovery of TMP269 and related compounds provides an alternative design for targeting metalloenzymes than the conventional chelating metal-binding group, and suggests a therapeutic potential for class IIa HDAC inhibitors distinct in mechanism and application compared to traditional HDAC inhibitors (e.g. TSA).
|Chemical Name:||N-((4-(4-phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl) |
|Solubility:||Up to 50 mM in DMSO|
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
|1.||Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. (2013) Nat Chem Biol. 9(5):319-25. Pubmed ID: 23524983|