FJ9

FJ9 (Compound 1) inhibits the interaction between GST-fused human NHERF1 PDZ1 domain and biotinylated β2AR carboxy-terminal peptide with an IC₅₀ of 1540 μM^[1].
FJ9 inhibits the interaction between GST-fused human NHERF1 PDZ2 domain and biotinylated CFTR carboxy-terminal peptide with an IC₅₀ of 160 μM^[1].
FJ9 (0.1-1000 μM) competitively inhibits Frz7 peptide binding to purified human DVL1 PDZ domain with a K_i of 63 μM and to purified human DVL3 PDZ domain with a K_i of 29 μM^[2].
FJ9 (100-300 μM; 24 hours) penetrates HEK293T cells and disrupts the intracellular interaction between HA-tagged mouse DVL1 and myc-tagged human Frz7 at concentrations of 100 μM and 300 μM^[2].
FJ9 (100-300 μM; 48 hours) dose-dependently down-regulates cytosolic β-catenin levels in hTERT-immortalized LP9 mesothelial cells stably expressing full-length mouse DVL1, but not in control LP9 cells or LP9 cells expressing PDZ domain-deleted mouse DVL1^[2].
FJ9 (100-300 μM; 24 hours) dose-dependently inhibits constitutive Tcf transcriptional activity in HCT116 p53^-/- colon cancer cells, reducing TOPflash reporter activity while minimally affecting FOPflash reporter activity^[2].
FJ9 (30-100 μM; 1-2 days) down-regulates canonical Wnt signaling target proteins (cyclin D1, c-myc, survivin) and mRNA (cyclin D1, survivin) in HCT116 p53^-/- colon cancer cells, and down-regulates survivin protein in NCI-H1703 non-small cell lung cancer cells^[2].
FJ9 (30-100 μM; 24 hours) does not affect JNK activation in mDVL1-transfected HeLa cells after 24 hours of treatment at 30 μM and 100 μM^[2].
FJ9 (86-100 μM; 3 to 6 days) induces significant apoptosis in LOX melanoma, NCI-H460 non-small cell lung cancer, and NCI-H1703 non-small cell lung cancer cells, but has no apoptotic effect on NCI-H28 mesothelioma cells or normal NHBE and SAEC cells, after 3 to 6 days of treatment at 86 to 100 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.