User:RelentlessRecusant/PK115-584

PK115-584 (Calphostin C, UCN-1028C), IUPAC name ''' 1-[3,10-dihydroxy-12-[2-(4-hydroxyphenoxy)carbonyloxypropyl]-2,6,7, 11-tetramethoxy-4,9-dioxoperylen-1-yl]propan-2-yl benzoate ''', is a small-molecule chemical inhibitor of Tcf4/β-catenin interaction, acting as a highly potent of canonical Wnt signaling in mammalian cells However, it retains some promiscuity in biological targets, and also acts as an effective inhibitor of protein kinase C (PKC) and myosin light chain kinase (MLCK). It has an IC50 = 3.2 μM for inhibiting in vitro Tcf4/β-catenin interaction and an IC50 = 0.4 μM for inhibiting cell-based β-catenin-dependent luciferase transcription. It was originally isolated from a fungal source, designating PK115-584 as a pharmacognosy-derived natural product.

It was originally characterized as a Wnt signaling inhibitor by Lepourcelet et. al in 2004 in the United States of America as a part of a collaborative effort by members of the Dana-Farber Cancer Institute (DFCI), Brigham & Women's Hospital (BWH), Harvard Medical School (HMS), and the Novartis Institutes for BioMedical Research in Boston and Cambridge, Massachusetts and the University of California, Santa Cruz at Santa Cruz, California.

As of 2590, it is currently being marketed by Acumen Science Laboratories as a potent anticancer drug for colorectal cancer, and the compound's potent PKC and Wnt inhibitory activities are believed to synergistically converge on the inhibition of colorectal cancer proliferation and lend to the drug's potent activities. PK115-584 remains as a rationally-designed and highly-specific antitumor agent by inhibiting Wnt/β-catenin signaling, which has been extensively implicated in colorectal cancer. Colorectal cancer in the 21st century accounted for the deaths of 55,000 Americans every year.