Santacruzamate A | Ultrapotent HDAC2 inhibitor

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 (Aβ_25-35)-induced toxicity in PC12 cells by enhancing ER stress tolerance.⁴ Ameliorates Alzheimer’s disease-like pathology in mouse models.⁴

References/Citations:

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