ZK824859 is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
ZK824859 hydrochloride is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
Phospholipase A2 (PLA2) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA2 (cPLA2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway. CAY10502 is a potent inhibitor of calcium-dependent cytosolic PLA2α (cPLA2α) with an IC50 value of 4.3 nM for the purified enzyme from human platelets. It inhibits arachidonic acid mobilization from A23187-stimulated or TPA-stimulated human platelets with IC50 values of 570 and 0.9 nM, respectively.
APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.
THR-18 is an 18-mer peptide derived from the sequence of human plasminogen activator inhibitor 1 (PAI-1), having the ability to bind to a site of tissue plasminogen activator (tPA) distal to its catalytic site and uncouple the beneficial clot-dissolving properties of tPA from its deleterious non-fibrinolytic effects.
3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg mL and a 50% inhibitory concentration (IC50) of 72.0microg mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).
Anwuweizonic acid may have inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice. Mixture of coccinic acid and anwuweizonic acid has antifertility activity, shows significant inhibitory activity against human decidu
Glochidiol exhibits strong inhibitory effects against all three human tumor cell lines (MCF-7, NCI-H-460 and SF-268), it exerts its antiproliferative activity through the involvement of apoptosis. It exhibits a strong inhibitory effect on mouse skin tumor
Karavilagenin D exhibits inhibitory effects on skin-tumor promotion in an in vivo two-stage mouse skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator, and with TPA as a promoter. It exhibits inhibition effect against human
Karounidiol exhibits cytotoxicity especially against a human renal cancer, it markedly suppresses the promoting effect of TPA (1 microgram/mouse) on skin tumor formation in mice following initiation with 7,12-dimethylbenz[a]anthracene (50 micrograms/mouse