FH535 is a Potent Inhibitor of Wnt/β-catenin and PPAR
The Wnt signaling pathway is important in normal development and in cancer. This signaling pathway is regulated by Wnt ligands, the APC-Axin complex and β-catenin. Wnt/β-catenin signaling pathway plays a central role in regulating the balance between stem cell growth and differentiation. Thus, the degree of Wnt signaling activation...
PX-12 is an Irreversible Inhibitor of Thioredoxin-1 (Trx-1)
Colorectal cancer is one of the leading causes of cancer-related mortality in most industrialized nations. It needs to find an effective adjuvant therapy for colorectal cancer. There includes non-steroidal anti-inflammatory drugs, immunotherapy, and gene therapy. Thioredoxin (Trx) and thioredoxin reductase 1 are among the major redox regulators in mammalian...
IACS-15414 is an Orally Active SHP2 Inhibitor
Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved structure and function. It has emerged as a key downstream regulator of several receptor tyrosine kinases (RTKs) and cytokine...
β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor
β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with DNA, which inhibits DNA replication,...
Troglitazone is an Orally Active PPARγ Agonist
Pancreatic cancer is the fourth leading cause of cancer-related deaths in Japan. Gemcitabine has been the standard therapy for advanced pancreatic cancer for over a decade. Additional novel combination therapies have been developed. It includes gemcitabine plus erlotinib; a combination of leucovorin, 5-fluorouracil, irinotecan, and oxaliplatin; and gemcitabine plus...
Cyclopamine is a Hedgehog (Hh) Pathway Antagonist
Hedgehog (Hh) signal pathway is a signal pathway that transmits information to embryonic cells for appropriate cell differentiation. Specifically, Hedgehog signaling pathway is one of the key regulators of animal development. There are three mammalian Hh proteins, Shh, Indian hedgehog (IHH), and desert hedgehog (DHH). Besides, Shh and IHH...
CX-5461 is an Orally Active rRNA Synthesis Inhibitor
RNA polymerase is an enzyme that synthesizes RNA from a DNA template. Specifically, RNA synthesis or transcription is the process of transcribing DNA nucleotide sequence information into RNA sequence information. Besides, RNA synthesis is catalyzed by a large enzyme called RNA polymerase. The basic biochemistry of RNA synthesis is...