SP-8356

SP-8356 is a derivative of (1S)-(–)-verbenone and an inhibitor of CD147, also known as extracellular matrix metalloproteinase (MMP) inducer (EMMPRIN) and previously known as tumor cell-derived collagenase stimulatory factor (TCSF).^1,2 It inhibits the dimerization of CD147 and the protein-protein interaction between CD147 and its ligand cyclophilin A. SP-8356 (10 µM) decreases recombinant human CD147-induced migration of A-10 vascular smooth muscle cells (VSMCs) and reduces cyclophilin A-induced increases in MMP-9 activity in, and adhesion of, isolated rat monocyte-derived macrophages. It also prevents glucose-oxygen deprivation-induced increases in reactive oxygen species (ROS) and lactate dehydrogenase (LDH) release in primary rat cortical neurons in an in vitro model of ischemia when used at a concentration of 10 µM.³ SP-8356 (5 µM) inhibits the migration and invasion of MDA-MB-231 breast cancer cells.⁴ In vivo, SP-8356 (50 mg/kg in the drinking water) decreases plaque size in an ApoE^-/- mouse model of atherosclerosis induced by partial carotid artery ligation and a high-fat diet.²

WARNING This product is not for human or veterinary use.

1. Pahk, K., Noh, H., Joung, C., et al. A novel CD147 inhibitor, SP-8356, reduces neointimal hyperplasia and arterial stiffness in a rat model of partial carotid artery ligation. J. Transl. Med. 17(1), 274 (2019).

2. Pahk, K., Joung, C., Song, H.Y., et al. SP-8356, a novel inhibitor of CD147-cyclophilin A interactions, reduces plaque progression and stabilizes vulnerable plaques in apoE-deficient mice. Int. J. Mol. Sci. 21(1), 95 (2019).

3. Ju, C., Song, S., Hwang, S., et al. Discovery of novel (1S)-(‒)-verbenone derivatives with anti-oxidant and anti-ischemic effects. Bioorg. Med. Chem. Lett. 23(19), 5421-5425 (2013).

4. Mander, S., Kim, D.H., Nguyen, H.T., et al. SP-8356, a (1S)-(‒)-verbenone derivative, exerts in vitro and in vivo anti-breast cancer effects by inhibiting NF-κB signaling. Sci. Rep. 9(1), 6595 (2019).