NP-G2-044 is a small molecule inhibitor of actin-bundling protein Fascin-1 (Fscn1), inhibits fascin-mediated actin bundling with IC50 of 0.2 uM.
Fascin (E391A mutant) (from the actin-binding site 1) is insensitive to the inhibition by NP-G2-044.
NP-G2-044 engages the target fascin and blocks filopodial formation in cells, decreases filopodial formation resulting in decreased lamellipodial formation.
NP-G2-044 inhibits the migration of MDA-MB-231 tumor cells with IC50 of ~10 uM.
NP-G2-044 (intraperitoneally and daily at 100 mg/kg) inhibits tumor metastasis on breast tumor metastasis in mouse models.
