SB-3CT 是一种可透过血脑屏障的、竞争性的金属蛋白酶MMP-2和MMP-9抑制剂,Ki分别为 13.9 nM、600 nM。他对明胶酶具有高选择性。它具有神经保护和抗癌作用。
产品描述
SB-3CT is a potent and specific gelatinase inhibitor for MMP-2(Ki=13.9 nM) and MMP-9(Ki=600 nM).
体外活性
在栓子引起的永久性脑缺血小鼠模型中,SB-3CT通过阻碍神经元层粘连蛋白的退化,保护神经元免受缺血性细胞死亡的损害.在L-CI.5sT细胞淋巴小鼠模型中,每天腹腔注射 SB-3CT(5-50 mg/kg),能够抑制肝癌细胞转移.在人前列腺癌细胞骨转移模型中,每天腹腔注射SB-3CT(50 mg/kg ),抑制细胞的生长,骨质溶解以及血管生成.
体内活性
SB-3CT能够降低溶骨性反应,有助于骨完整性的保持。在PC3肿瘤细胞中,SB-3CT抑制细胞的生长。在基底膜基质中,SB-3CT直接抑制骨髓内皮细胞浸润和小管形成。
激酶实验
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.
细胞实验
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].
Cas No.
292605-14-2
分子式
C15H14O3S2
分子量
306.39
储存和溶解度
DMSO:30.6 mg/mL (100 mM)
Ethanol:6.1 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years