TM5441

SKU: orb1222826

Description

TM-5441, also known as EBP 883 and BMS-790052, is a potent plasminogen activator inhibitor-1 (PAI-1). TM-5441 inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM. TM5441 protects against high-fat diet-induced obesity and adipocyte injury in mice.

Key Properties

• CAS Number: 1190221-43-2
• MW: 428.83
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₇ClN₂O₆
• SMILES: O=C(O)c3cc(Cl)ccc3NC(=O)COCC(=O)Nc1cccc(c1)c2ccco2
• Target: PAI-1
• Solubility: DMSO : ≥ 300 mg/mL; 699.59 mM

Bioactivity

• In Vivo:
  Oral administration of TM5441 (20 mg/kg daily) 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. The average peak plasma concentration is 11.4 μM one hour after oral administration and undetectable levels 23 hours after administration. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence, prolongs lifespan in klotho null mice and elicits anti-tumorigenic and anti-angiogenic activities in cancer.
• In Vitro:
  TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 13.9 and 51.1 μM. 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. TM5441 induces mitochondrial depolarization. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TM-5441 | BMS790052 | EBP883

Quick Database Links

Gene Symbol

PAI-1