Verrucarin A | Steroid receptor coactivator-3 inhibitor

Verrucarin A (3148-09-2) is a macrocyclic trichothecene mycotoxin from Myrothecium sp. It is a potent and selective inhibitor of the steroid receptor coactivator-3 and selectively down-regulates its expression.¹ It is cytotoxic to multiple types of cancer cells at low nM concentrations (IC₅₀=4.9 nM for HepG2 cells) but not toward normal liver cells.^1,2 It enhances TNFα-induced³ and TRAIL-induced apoptosis⁴. It reduces phosphorylation of IREα and inhibits tunicamycin-induced ER stress in FaO rat liver cells.⁵

References/Citations:

1. Yan et al. (2014), Identification of verrucarin A as a potent and selective steroid receptor coactivator-3 small molecule inhibitor; PLoS One, 9 e95243
2. Palanivel et al. (2014), Verrucarin A alters cell-cycle regulatory proteins and induces apoptosis through reactive oxygen species-dependent p38MAPK activation in the human breast cancer cell line MCF-7; Tumour Biol., 35 10159
3. Jayasooriya et al. (2013), Combined treatment with verrucarin A and tumor necrosis factor-α sensitizes apoptosis by overexpression of nuclear factor-kappaB-mediated Fas; Environ. Toxicol. Pharmacol., 36 303
4. Moon et al. (2013), Verrucarin A sensitizes TRAIL-induced apoptosis via the upregulation of DR5 in an eIF2α/CHOP-dependent manner; Toxicol. In Vitro, 27 257
5. Bae et al. (2016), Inhibitory Effects of Verrucarin A on Tunicamycin-Induced ER Stress in FaO Rat Liver Cells; Molecules, 20 8988