JavaScript seems to be disabled in your browser. For the best experience on our site, be sure to turn on Javascript in your browser.
Tel: +1-832-696-8203
Email: [email protected]
Worldwide Distributors
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ML161 is a selective inhibitor of PAR1 with IC50 value of 0.26 μM [1].
Protease-activated receptor-1(PAR-1) is a unique G-protein-coupled receptor belonging to the protease-activated receptor family and its activation leads to downstream signaling events that launch a variety of cellular responses related to tumor progression [1].
ML161 is a potent PAR1 inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with human platelets, ML161 treatment inhibited the activation of thrombin-induced platelet in a dose-dependent manner by detecting P-selectin expression [1]. When tested with granule secretion, ML161 exhibited a potent inhibition on P-selectin expression in a dose-dependent manner with EC50 value of 0.3μM and also inhibited SFLLRN-induced thrombus formation [2].
References: [1]. Dockendorff, C., et al., Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett, 2012. 3(3): p. 232-237.[2]. VerPlank, L., et al., Chemical Genetic Analysis of Platelet Granule Secretion-Probe 3, in Probe Reports from the NIH Molecular Libraries Program. 2010, National Center for Biotechnology Information (US): Bethesda (MD).
