ACT001(DMAMCL, dimethylaminomicheliolide) is a PAI-1 inhibitor and exerts antitumor effects on neuroblastoma (NB) both in vitro and in vivo. It also exerts synergistic effects in combination with cisplatin through the inhibition of the PAI-1/PI3K/AKT pathway.

WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibit 10 Units of human uPA with IC50 of 90 nM.

WX-293 is a highly selective small-molecule inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 2.4 uM.

IPR3011 is a small-molecule uPAR-uPA protein-protein interaction inhibitor with Ki of 2.4 uM.

ACT001 is orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of Micheliolide, can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.

TM5441 is a novel orrally active TAP-1 antagonist.

TM5275 is an orally available, potent and selective inhibitor of PAI-1 that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates.

Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor drug candidate. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)-induced diabetes. Cenupati

UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

WX-UK1 (UKI-1) is a small synthetic serine protease uPA (urokinase-type plasminogen activator) inhibitor that blocks tumor cell invasion, metastasis and primary tumor growth.

Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).

ZK824859 is a selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.

28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator inhibitor with IC50 at 37.82 μM.

Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy.

UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion.

Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.