As　a　trypsin-like　serine　protease,　Urokinase-type　plasminogen　activator　(uPA)　plays　a　key　role　in　a　range　of　biological　processes　including　plasminogen　activation,　angiogenesis,　wound　healing,　tissue　remodeling,　tumor　growth　and　tumor　metastasis.　uPA　is　shown　as　the　most　validated　marker　for　prognosis　of　breast　cancer.　Inhibitors　of　uPA　may　then　be　useful　in　the　treatment　of　cancer　by　retarding　tumor　growth　and　metastasis.　Most　current　uPA　inhibitors　employ　a　highly　basic　group　(amidine　or　guanidine　group)　to　target　the　primary　specific　pocket　of　uPA　active　site,　which　leads　to　poor　oral　bioavailability.　Here,　a　uPA　inhibitor　with　weak　basic　P1　group,　2-(2-aminobenzothiazole-6-carboxamido)　acetic　acid　(ABTCA),　was　synthesized　and　reported　here.　In　addition,　we　also　determined　the　crystal　structure　of　ABTCA　in　complex　with　uPA.　The　structural　information　will　be　useful　for　further　improvements　of　potency　and　selectivity　of　this　promising　new　type　of　uPA　inhibitors.