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.
