SDCBP Inhibitor

PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer.

SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC₅₀ value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research.

IVMT-Rx-3 is a inhibitor of SDCBP targeting of the PDZ1 and PDZ2 Domains of MDA-9/Syntenin. IVMT-Rx-3 blocks MDA-9/Syntenin interaction with Src, reduces NF-κB activation, and inhibits MMP-2/MMP-9 expression. IVMT-Rx-3 inhibits Melanoma Metastasis^[1]

KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin.