Santacruzamate A (CAY10683)

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.