MO-I-1100

MO-I-1100 is a **small molecule inhibitor** that selectively targets the β-hydroxylase activity of **aspartate β-hydroxylase (ASPH)**, an enzyme overexpressed on the surface of various tumor cells. MO-I-1100 directly inhibits ASPH enzymatic activity by approximately 80%, leading to suppressed tumor cell migration, invasion, and growth, particularly in cancers with high ASPH expression, such as hepatocellular carcinoma (HCC) and pancreatic cancer (PC)[1][2][3]. MO-I-1100's anti-tumor effects are linked with downregulation of **Notch signaling**: treatment leads to reduced expression of Notch1 intracellular domain (ICN), Notch ligands (such as Jagged 2), and downstream Notch-responsive genes (including HES1, HEY1, EpCAM, CD44, c-Myc, MMP2/9, cyclin D3, and PCNA)[1][2][3]. Its efficacy has been demonstrated in vitro and in vivo, where intraperitoneal administration in xenograft mouse models significantly inhibited tumor growth and progression, without notable toxicity[1][3]. MO-I-1100 appears particularly effective in tumors with high ASPH overexpression, while its effect is minimal in cells/tumors with low ASPH expression[2][3]. The compound was developed using high-throughput screening and structure-based design for specific ASPH β-hydroxylase inhibition[3].

Brand names

MO-I-1100MO-I1100MO-I 1100

Other names

MO-I-1100MO-I1100MO-I 1100