STA-21 is a natural antibiotic that potently inhibits STAT3 by preventing its dimerization and DNA binding when used at concentrations of 20-30 µM. It blocks the growth and survival of cancer cells that express constitutively active STAT3 (e.g., DU145 cells, IC50 = 12.2 µM). STAT3 inhibitors, including STA-21,...

PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki = 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein. It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite. The prominent...

JNK inhibitor VIII is an inhibitor of JNK1, JNK2, and JNK3 (Kis= 2, 4, and 52 nM, respectively). It is selective for JNK1, JNK2, and JNK3 over a panel of 74 kinases (Kis = >720 nM for all). It inhibits the phosphorylation of c-Jun in HepG2 cells (EC50 = 920 nM). JNK inhibitor VIII (10 µM) inhibits NGF-induced...

SU 9516 is a 3-substituted indolinone that has anti-proliferative and pro-apoptotic activity in tumor cells. It is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1). It does not inhibit PKC, p38,...

CL 316,243 is a beta3-adrenoceptor agonist (EC50 = 3 nM) that is >10,000-fold selective over beta1 and beta2. It causes a rapid decrease in blood glucose level in mice and has been used to study the induction of brown adipocytes and to increase thermogenesis in a mouse model of dietary obesity.Formal Name:...