VT-103

VT-103 is a small molecule, orally bioavailable, and selective inhibitor of the Transcriptional Enhancer Associate Domain 1 (TEAD1) protein. It specifically targets TEAD1 auto-palmitoylation, a post-translational modification essential for TEAD transcriptional activity. By blocking this process, VT-103 disrupts the interaction between TEAD and its co-activators YAP (Yes-associated protein) and TAZ (Transcriptional co-activator with PDZ-binding motif), thereby inhibiting the Hippo signaling pathway-driven gene transcription. The compound demonstrates high selectivity for TEAD1 over other family members (TEAD2, TEAD3, and TEAD4). It has shown significant preclinical anticancer activity in models of NF2-deficient or NF2-mutated mesothelioma. Currently, VT-103 is primarily utilized as a research tool compound and is not approved for human use.

Other names

CAS 2290608-13-6CAS2290608-13-6CAS-2290608-13-6