CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 µM.1 Similar potency is observed with trapoxin A and B, whereas trichostatin A is more potent inhibitor of the enzyme. Trichostatin A also selectively inhibits the removal of acetyl groups from the amino-terminal lysine residues of core histones, which modulates the access of transcription factors to the underlying genomic DNA.2 However, trichostatin A is much more expensive than CAY10398. CAY10398 thus represents a selective and cost-effective compound for the inhibition of HDAC.
1
Jung, M., Hoffmann, K., Brosch, G., et al. Analogues of Trichostatin A and Trapoxin B as histone deacetylase inhibitors. Bioorg Med Chem Lett71655-1658(1997).
2
Taunton, J., Hassig, C.A., and Schreiber, S.L. A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p. Science272408-411(1996).
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ONC(=O)CCCCCNC(=O)c1ccc(cc1)N(C)C
Background Reading
Taunton, J., Hassig, C.A., and Schreiber, S.L. A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p. Science272408-411(1996).
Jung, M., Hoffmann, K., Brosch, G., et al. Analogues of Trichostatin A and Trapoxin B as histone deacetylase inhibitors. Bioorg Med Chem Lett71655-1658(1997).
CAY10398 is available in the following screening
libraries: