The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM). This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM). CAY10561 inhibits proliferation of COLO205 cells with an IC50 value of 0.54 μM.
Taiwanhomoflavone A is cytotoxic with ED50 values of 3.4, 1.0, 2.0 and 2.5 microg ml, respectively, against KB epidermoid carcinoma of nasopharynx, COLO-205colon carcinoma, Hepa-3B hepatoma, and Hela cervix tumor cells.
DC1 is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065. DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer. DC1Sme is a DC1 derivative with IC50 values of Ramos, Namalwa, HL60 / s
Pyracrenic acid is a potent elastase inhibitor with an IC50 value of 1.5 mg mL. Pyracrenic acid shows DPPH radical scavenging activity. It also shows significant cytotoxic activities against human cancer cells COLO205 and AGS.