CEP-1347

CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53^{[1][2][3][4][5][6]}. In Vitro:CEP-1347 (0-500 nM; 3 days) decreases the expression of MDM4 and activates the p53 pathway in malignant meningioma cells with wild-type p53^[4].
CEP-1347 (KT7515) promotes motor neuron survival by inhibiting JNK1 activity in rat embryonic motor neurons deficient in nutritional factors. The IC₅₀ values of CP-1347 for JNK1 activation and EC₅₀ values of motor neuron survival are both 20 nM^[5].
CEP-1347 (0.2-20 μM; 2 h) dose-dependently inhibits pancresin-induced JNK activation in isolated pancreatic acinus, and is almost completely effective at a concentration of 2 μM^[6].
In Vivo:CEP-1347 (0-60 mg/kg; Subcutaneous injection (s.c.)) in rats treated with Caerulein (HY-A0190) (10 μg/kg; Intravenous injection (i.v.)) can dose-dependent inhibit Caerulein Induced JNK activation and improve pancreatitis induced by pancreatin^[6].