<p>Protein kinase C (PKC) is a family of serine-threonine kinases with various subclasses. There is mounting proof that PKCs are essential for the emergence of cancer. Interestingly, PKCs have been receiving a lot of attention because they have both stimulatory and inhibitory effects on the development and proliferation of cancerous cells. PKC inhibitors have emerged as a promising cancer therapeutic target due to their capacity to influence a variety of cellular processes related to developing cancer and progression. PKC inhibitors fall into three general categories: anti-sense oligonucleotides, biological modulators, and tiny-molecule inhibitors. By interfering with PKC’s capacity to bind to its substrates or targeting particular PKC isoforms, these inhibitors can interfere with downstream signaling cascades. H-7, known to inhibit PKC, as well as it can also inhibit other kinases such as cAMP-dependent protein kinase (PKA) and cGMP-dependent protein kinase (PKG). Its anticancer responses to cancer cells have been extensively researched. Here, we thoroughly examine the most recent developments in the structure, regulation, and biological roles of H-7, an inhibitor of PKCs, with a focus on H-7’s connection to death of cells brought on by anti-cancer therapy and the current understanding of H-7 role in tumor metabolism. Additionally, we go over how basic studies a suggest that H-7 may be an objective for therapeutic approach in cancer.</p>