SB-3CT is a potent and specific gelatinase inhibitor for MMP-2 (Ki = 13.9 nM) and MMP-9 (Ki = 600 nM).

MMP2:13.9 nM(Ki), MMP9:600 nM(Ki)

In a permanent cerebral ischemia mouse model induced by an embolus, SB-3CT protects neurons from ischemic cell death by inhibiting the degradation of neuronal adhesion proteins. Furthermore, daily intraperitoneal injections of SB-3CT (5-50 mg/kg) in the L-CI.5sT murine lymphoma model significantly hinders liver cancer cell metastasis. Likewise, in a model of osteolytic metastasis of human prostate cancer cells, daily intraperitoneal administration of SB-3CT (50 mg/kg) curtails cell growth, bone resorption, and angiogenesis.

SB-3CT is capable of reducing osteolytic responses, aiding in the maintenance of bone integrity. In PC3 tumor cells, SB-3CT inhibits cellular growth. Within the basement membrane matrix, SB-3CT directly suppresses the infiltration of bone marrow endothelial cells and tubule formation.

kinase assays: PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1?μM ATP. The kinase reaction is carried out for 1?hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10?μM ATP.

SB-3CT is dissolved in DMSO (10 mM) and stored (-22°C), and then diluted with appropriate media (DMSO 1%) before use[2]. PC3 cells are seeded in 35-mm dishes (5×104 cells/dish) in complete culture medium. The next day, the medium is replaced with complete medium supplemented with 1% DMSO alone (vehicle) or SB-3CT (final concentrations 0.1-50 μM) in 1% DMSO. At various times, the cells are harvested with trypsin and counted[2].

Ethanol: 6.1 mg/mL (19.91 mM), Sonication is recommended.

DMSO: 250 mg/mL (815.93 mM), Sonication is recommended.