CRT0044876 is a Potent and Selective APE1 Inhibitor

The base excision repair (BER) pathway is essential for the removal of DNA bases damaged by alkylation or oxidation. This pathway also handles a variety of other lesions including deaminated bases and DNA single-strand breaks. A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate...

Z-LEHD-FMK is a Selective and Irreversible Inhibitor of Caspase-9

TRAIL is a potent inducer of apoptosis of transformed and cancer cells but not of most normal cells. TRAIL induces apoptotic death on binding to either of two proapoptotic TRAIL receptors, TRAIL R1 or TRAIL R2. Moreover, normal cells may resistant to TRAIL because of expressing higher levels of...

RJW100 is a Potent LRH-1 and SF-1 Agonist

Liver receptor homolog 1 (LRH-1, NR5A2) is a member of the nuclear receptor family. Specifically, LRH-1 plays a key role in regulating development, cholesterol transport, bile acid homeostasis, and steroid production. Besides, LRH-1 regulates hepatobiliary acid biosynthesis and cholesterol homeostasis and is the main controller of hepatobiliary. Therefore, the...

CAY10404 is a Highly Selective COX-2 Inhibitor

Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...

IPI-9119 is an Orally Active, Selective and Irreversible FASN Inhibitor

Fatty acid synthase (FASN) is a multi-enzyme protein that catalyzes the synthesis of fatty acids. Its main function is to catalyze the synthesis of palmitate (C16:0) from acetyl CoA and malonyl COA in the presence of NADPH. Specifically, FASN is a key enzyme responsible for the synthesis of fatty...

SM1-71 is a Multi-Targeted Kinase Inhibitor with Anti-Cancer Activity

In this article, we will introduce a potent TAK1 inhibitor, with a Ki of 160 nM. SM1-71 inhibits MEK1 activities with an IC50 of 142 nM. It also exhibits only weak activity against ERK2 with an IC50 of 1090 nM. Additionally, SM1-71 has an acrylamide warhead in the ortho-position. At the same time, it...