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Src inhibitors act on the Src family of non-receptor tyrosine kinases, which relay receptor and adhesion signals. Cellular Src (c-Src) is kept inactive when its Src homology 2 (SH2) domain binds a phosphorylated tyrosine in its C-terminal tail. Src family kinases regulate cell adhesion, migration, proliferation and survival, and they also transmit signals from immune receptors. Dasatinib, bosutinib and saracatinib inhibit both Src and the Abelson tyrosine kinase (Abl). PP2, a pyrazolopyrimidine compound, is a widely used Src family inhibitor in cell signaling studies. Tirbanibulin, first reported as KX2-391, is a further Src inhibitor in this category.
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase, acting through CRBN-mediated ubiquitination. It effectively reduces c-Src levels and inhibits proliferation in c-Src-dependent cancer cell lines, making it a useful tool for targeted protein degradation research.
SB1-G-187 is a multifunctional PROTAC designed as a multi-kinase degrader, capable of inducing the selective degradation of multiple kinase targets through the ubiquitin–proteasome system. In addition to its targeted degradation activity, SB1-G-187 features an alkyne functional group, enabling its use as a click chemistry reagent. It can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, allowing for versatile applications in chemical biology, such as probe development, conjugation, and target identification.
ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis.
