Description
NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).1,2 It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.1 NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.2 NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.3WARNING This product is not for human or veterinary use.
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