Downregulate phosphorylation of STAT3, increase the expression of cleavedcaspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.
Lig4-4 is a TREK-1 current inhibitor (IC50 = 2.06 μM) that has demonstrated potential for use as a protective agent against cerebral ischemia. It has been postulated that the neuroprotective effects of Lig4-4 against cerebral ischemia may be attributed to the modulation of Bcl-2 and cleaved-caspase-3 expression, leading to the inhibition of neuronal apoptosis.
Myrothecine A, a trichothecene mycotoxin discovered in M. roridum, exhibits anticancer properties. It effectively inhibits the proliferation of various cancer cell lines, specifically A549, MCF-7, HepG2, and SMMC-7721, with IC50 values of 95, 70, 60, and 25 µM, respectively. At a concentration of 50 µM, Myrothecine A induces G1 cell cycle arrest in HepG2 cells and promotes apoptosis in SMMC-7721 cells by elevating levels of Bax and cleavedcaspase-3, -5, and -8.