notch3

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

NSC 405020 is a noncatalytic inhibitor of MT1-MMP.

Notch inhibitor 1 is an effective Notch inhibitor (IC50s: 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively). Notch inhibitor 1 is also used in the research of cancer.

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.

S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells when xenotransplanted into mice.

Tarextumab (OMP-59R5) is a fully human IgG2 monoclonal antibody designed to selectively target and inhibit the signaling of Notch2 and Notch3 receptors. preclinical and clinical studies have demonstrated that inhibition of the Notch2/3 pathway with chemotherapeutic agents is efficacious across a broad spectrum of epithelial tumors, including breast, lung, ovarian, and pancreatic cancers, thereby establishing Tarextumab as a promising candidate for oncological research and development.