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TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), with IC50 values between 13.9 and 51.1 μM against several human cancer cell lines. TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441 increases apoptosis in HT1080 and HCT116 cells.
In vivo, TM5441 (20 mg/kg/day; Oral) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival.
| Molecular Weight | 428.82 |
| Formula | C21H17ClN2O6 |
| CAS Number | 1190221-43-2 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PAI-1 Products |
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| PAI-039
PAI-039 is an inhibitor of plasminogen activator inhibitor-1 (PAI-1). |
| Loureirin B
Loureirin B is a flavonoid isolated from The blood tree of Pterygophyllum SPP. It is an inhibitor of PAI-1 with IC50 value of 26.10 μM. Loureirin B can inhibit the phosphorylation of KATP, ERK and JNK at the same time, showing an anti-diabetes effect. |
| TM5275 sodium salt
TM5275 sodium is an orally available, potent and selective plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates. |
| Toddalolactone
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM. |
| AZ3976
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay. |
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