PDZ1i

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[1][2][3].

Product Specifications

CAS Number

[2083618-79-3]

Product Name Alternative

113B7

UNSPSC

12352005

Hazard Statement

H315, H319

Target

EGFR; FAK; MMP; NF-κB; SDCBP

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Metabolic Enzyme/Protease; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pdz1i.html

Purity

99.29

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N2C(NC3=C1CCC3)=NC(C(NC(C=C4C)=C(C=C4NC(CCC5=NN=C(C6=CC=CC=C6)O5)=O)C)=O)=N2

Molecular Formula

C28H26N8O4

Molecular Weight

538.56

Precautions

H315, H319

References & Citations

[1]Kegelman TP, et al. Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin. Proc Natl Acad Sci U S A. 2017 Jan 10;114 (2) :370-375.|[2]Das D, et al. Suppression of Prostate Cancer Pathogenesis Using an MDA-9/Syntenin (SDCBP) PDZ1 Small-Molecule Inhibitor. Mol Cancer Ther. 2019 Nov;18 (11) :1997-2007.|[3]Clark GC, et al. Radiation induces ESCRT pathway dependent CD44v3+ extracellular vesicle production stimulating pro-tumor fibroblast activity in breast cancer. Front Oncol. 2022 Aug 29;12:913656.