A histone deacetylase inhibitor
Santacruzamate A (CAY10683) is a potent and selective inhibitor of histone deacetylase with IC50 values of 0.112 and 433 nM for HDAC2 and HDAC6, respectively [1].
Histone deacetylases (HDACs) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.
Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor. Natural and synthetic santacruzamate A inhibited HDAC2 with IC50 values of 119 and 112 pM respectively and inhibited HDAC6 with IC50 values of 434 and 433 nM, respectively. Santacruzamate A was 700-fold more potent than SAHA for HDAC2. However, santacruzamate A inhibited HDAC4 with IC50 values of >1 μM. In HCT-116 colon carcinoma cells, natural and synthetic santacruzamate A inhibited cell growth with GI50 values of 29.4 and 28.3 μM, respectively. In HuT-78 cutaneous T-cell lymphoma cells, both inhibited cell growth with GI50 values of 1.4 and 1.3 μM, respectively [1].
Reference:
[1].? Pavlik CM, Wong CY, Ononye S, et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J Nat Prod, 2013, 76(11): 2026-2033.
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