GSK2334470

GSK2334470 is a highly specific and potent **inhibitor of PDK1 (3-phosphoinositide-dependent protein kinase-1)**, with an IC50 of approximately 10 nM for PDK1[1]. It exhibits minimal activity against a broad panel of other kinases, including Aurora, ROCK, p38 MAPK, and PI3K[1]. **Mechanistically, GSK2334470 blocks the phosphorylation of multiple PDK1 substrates, such as SGK, S6K1, RSK, and Akt1, and inhibits the activation of the downstream PI3K/Akt/mTOR signaling pathway**[1][2][3][5]. This inhibition results in suppressed proliferation and induced apoptosis in various cancer cell lines, including renal cell carcinoma (RCC)[2] and multiple myeloma (MM)[3][5]. GSK2334470 demonstrates antitumor activity both in vitro and in xenograft tumor models and is well-tolerated[2][3][5]. **GSK2334470 is a research compound originally developed by GSK (GlaxoSmithKline) and is used to evaluate the role of PDK1 signaling in cancer and other diseases.** It is not approved for clinical use.

Other names

GSK470GSK-470GSK 4701227911-45-6