| 名稱 | SB-3CT |
| 描述 | SB-3CT is a potent and specific gelatinase inhibitor for MMP-2(Ki=13.9 nM) and MMP-9(Ki=600 nM). |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在栓子引起的永久性腦缺血小鼠模型中,SB-3CT通過阻礙神經(jīng)元層粘連蛋白的退化,保護(hù)神經(jīng)元免受缺血性細(xì)胞死亡的損害.在L-CI.5sT細(xì)胞淋巴小鼠模型中,每天腹腔注射 SB-3CT（5-50 mg/kg）,能夠抑制肝癌細(xì)胞轉(zhuǎn)移.在人前列腺癌細(xì)胞骨轉(zhuǎn)移模型中,每天腹腔注射SB-3CT（50 mg/kg ）,抑制細(xì)胞的生長,骨質(zhì)溶解以及血管生成. |
| 體內(nèi)活性 | SB-3CT能夠降低溶骨性反應(yīng),有助于骨完整性的保持。在PC3腫瘤細(xì)胞中,SB-3CT抑制細(xì)胞的生長。在基底膜基質(zhì)中,SB-3CT直接抑制骨髓內(nèi)皮細(xì)胞浸潤和小管形成。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 6.1 mg/mL (19.91 mM), Sonication is recommended.
10% DMSO+90% (20% SBE-β-CD in Saline) : < 10 mg/mL (32.64 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 250 mg/mL (815.93 mM), Sonication is recommended.
10% DMSO+90% Corn oil : < 10 mg/mL (32.64 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% Saline : < 10 mg/mL (32.64 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 10 mg/mL (32.64 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
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| 關(guān)鍵字 | SB-3CT | SB3CT | SB 3CT | permeability | neuroprotective | MMP-9 | MMP-2 | MMP | metalloproteinase | Matrix metalloproteinases | matrix | Inhibitor | inhibit | gelatinases | effects | blood-brain | barrier | anticancer |
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