CTS-1027 is a selective inhibitor of MMP with IC50 value of 0.4 nM for MMP 2 and 0.6 nM for MMP13 [1]. MMPs (matrix metalloproteinase) are zinc-dependent endopeptidases and play an important role in degrading all kinds of extracellular matrix proteins. It is well known that MMPs involve in the cleavage of cell surface receptors, the release of apoptotic ligands, and inactivation chemokine/cytokine. And MMPs also play a pivotal role in cell proliferation, migration, differentiation, angiogenesis, apoptosis and host defense [2] [3]. In C57/BL6 mice model suffered bile duct ligation (BDL) for 14 days, gavage CTS-1027 reduced apoptosis of hepatocyte and bile infarcts which was a histologic indicator of liver injury at the same time activated stellate cells and reduced hepatic fibrogenesis [4]. References: [1]. Barta, T.E., et al., Selective, orally active MMP inhibitors with an aryl backbone. Bioorg Med Chem Lett, 2001. 11(18): p. 2481-3. [2]. Toth, M., A. Sohail, and R. Fridman, Assessment of gelatinases (MMP-2 and MMP-9) by gelatin zymography. Methods Mol Biol, 2012. 878: p. 121-35. [3]. Roomi, M.W., et al., Patterns of MMP-2 and MMP-9 expression in human cancer cell lines. Oncol Rep, 2009. 21(5): p. 1323-33. [4]. Kahraman, A., et al., Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res, 2009. 39(8): p. 805-13.
Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips
We do not recommend long-term storage for the solution, please use it up soon.
Biological Activity
Description
CTS-1027 is an orally bioavailable and small-molecule inhibitor of matrix metalloproteinases (MMPs) with IC50 values of 0.4 nM, 0.6 nM and 800 nM for MMP-2, MMP-13 and MMP-1, respectively.
