Santacruzamate A
HDAC2 inhibitor / 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 A fragment (A25-35)-induced toxicity in PC12 cells by enhancing ER stress tolerance.4 Ameliorates Alzheimer’s disease-like pathology in mouse models.4
Biochemicals & reagents
1477949-42-0
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
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TARGET: Protein deacetylase -- PATHWAY: Chromatin; Apoptosis inducer; Posttranslational modification -- RESEARCH AREA: Epigenetics; Cell death; Cellular stress; Neuroscience -- DISEASE AREA: Neurodegeneration; Cancer