ITD1

ITD1 is a selective small molecule inhibitor of the Transforming Growth Factor-Beta (TGF-β) signaling pathway. It functions by specifically binding to the TGF-beta receptor type 2 (TGFBR2) and inducing its proteasomal degradation, which effectively clears the receptor from the cell surface and inhibits downstream SMAD2/3 signaling. Originally identified through a high-throughput screen for its ability to promote the differentiation of cardiomyocytes from human pluripotent stem cells, ITD1 has more recently been investigated as a potential therapeutic for aggressive cancers such as glioblastoma (GBM). In preclinical models of recurrent GBM, ITD1 has demonstrated the ability to reduce cancer stem cell capacity and re-sensitize tumor cells to temozolomide, although its efficacy in orthotopic brain models is often limited by the rapid acquisition of resistance.

Other names

ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate