Tilmicosin is a macrolide antibiotic. It is active against macrolide-susceptible strains of M. haemolytica, P. multocida, and E. coli (MICs = 4, 4, and 128 µM, respectively), as well as a hyperpermeable strain of E. coli (MIC = 2 µM), and inhibits bacterial protein synthesis (IC50 = 0.36 µM). Tilmicosin (75 mg/kg)...

The calpains are a family of calcium-dependent cysteine proteases, with calpain I (µ-calpain) requiring micromolar calcium and calpain II (m-calpain) requiring millimolar calcium. Suc-Leu-Tyr-AMC is a fluorescent substrate for calpain I and II and papain (another cysteine protease) that is used for measuring the...

Irinotecan, a derivative of the alkaloid camptothecin (Cay-11694), functions as a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I. Its action is terminated by glucuronidation by UDP glucuronosyl transferase 1A1. Irinotecan demonstrates...

ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression. It is inactive at the related steroidogenic factor-1 transcriptional activator. Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the...

Two Rho-associated kinases (ROCKS), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK...