| Bioactivity | TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence[1][2]. | ||||||||||||
| Invitro | TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 13.9 and 51.1 μM[1].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[1].TM5441 induces mitochondrial depolarization[1].In mouse proximal tubular epithelial cells, TM5441 effectively inhibits PAI-1-induced mRNA expression of fibrosis and inflammation markers and also reverses PAI-1-induced inhibition of plasmin activity[2]. | ||||||||||||
| Name | TM5441 | ||||||||||||
| CAS | 1190221-43-2 | ||||||||||||
| Formula | C21H17ClN2O6 | ||||||||||||
| Molar Mass | 428.82 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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