notch3

BMS-906024 (Osugacestat) 是一种可口服且具有选择性的γ 分泌酶抑制剂，是一种小分子 Notch 抑制剂。BMS-906024 对多种人类癌症异种移植具有广谱抗肿瘤活性。BMS-906024 可阻止所有四种 Notch 受体的激活，对 Notch1、-2、-3 和 -4 受体的 IC50 分别为 1.6、0.7、3.4 和 2.9 nM。

NSC 405020 是一种 MT1-MMP 的非催化抑制剂，可特异地靶向 MT1-MMP 的 PEX 结构域，不会抑制 MT1-MMP 和 MMP-2的催化活性。

Anti-NOTCH3 Antibody 是一种 CHO 表达的人源抗体，靶向 NOTCH3，配有 huIgG1 型重链和 huκ 型轻链。其预测分子量 (MW) 为 150 kDa。Anti-NOTCH3 Antibody 的同型对照可参考 HumanIgG1kappa, Isotype Control。

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.