Biochemicals & reagents
1) Pavlik et al. (2013), Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.; J. Nat. Prod., 76 2026 2) Zhou et al. (2018), Pharmacological or transcriptional inhibition of both HDAC1 and 2 leads to cell cycle blockage and apoptosis via p21Waf1/Cip1 and p19INK4d upregulation in hepatocellular carcinoma; Cell Prolif., 51(3) e12447 3) Damaskos et al. (2017), Histone Deacetylase Inhibitors: An Attractive Therapeutic Strategy Against Breast Cancer; Anticancer Res., 37 35 4) Chen et al. (2019), Santacruzamate A Ameliorates AD-Like Pathology by Enhancing ER Stress Tolerance Through Regulating the Functions of KDELR and Mia40-ALR in vivo and in vitro; Front. Cell. Neurosci., 13 61
Santacruzamate A is a highly potent and selective inhibitor of HDAC2 isolated from the Panamanian marine cyanobacterium cf. Symploca (IC50=0.119 and 434 nM for HDAC2 and HDAC6 respectively) (1). This compound induces apoptosis and cancer cell death only in combination with other HDAC1 inhibitors (2). It is also a potential therapeutic agent for breast cancer (3), it attenuates the Aβ fragment (Aβ25-35)-induced toxicity in PC12 cells by enhancing ER stress tolerance (4). It ameliorates Alzheimer’s disease-like pathology in mouse models (4).