Description
Santacruzamate A (1477949-42-0) 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?Induces apoptosis and cancer cell death only in combination with other HDAC1 inhibitors.2?Potential therapeutic agent for breast cancer.3?Attenuates Aβ fragment (Aβ25-35)-induced toxicity in PC12 cells by enhancing ER stress tolerance.4?Ameliorates Alzheimer’s disease-like pathology in mouse models.4
References
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
