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SW033291 是有效的15-PGDH 抑制剂,与15-PGDH 亲和力高,Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。
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SW033291 是有效的15-PGDH 抑制剂,与15-PGDH 亲和力高,Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 297 | 现货 | |
2 mg | ¥ 439 | 现货 | |
5 mg | ¥ 719 | 现货 | |
10 mg | ¥ 1,170 | 现货 | |
25 mg | ¥ 2,190 | 现货 | |
50 mg | ¥ 3,260 | 现货 | |
100 mg | ¥ 4,770 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 655 | 现货 |
产品描述 | SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues. |
靶点活性 | 15-PGDH:0.1 nM(Ki), 15-PGDH:1.5 nM |
体外活性 | 在Vaco-503细胞中,SW033291 (2.5 μM) 通过降低85%的细胞内15-PGDH酶活性。[1] |
体内活性 | 在接受骨髓移植的小鼠中,SW033291(10 mg/kg,腹腔注射)促进了血液生成的恢复。在结肠和肝脏损伤的小鼠模型中,SW033291(10 mg/kg,腹腔注射)降低了与结肠炎相关的炎症细胞因子的水平,保护小鼠不受结肠炎影响,并促进了肝脏再生。[1] |
激酶实验 | Fluorescence anisotropy (FP) ligand displacement assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM). |
分子量 | 412.59 |
分子式 | C21H20N2OS3 |
CAS No. | 459147-39-8 |
Smiles | CCCCS(=O)c1sc2nc(cc(-c3ccccc3)c2c1N)-c1cccs1 |
密度 | no data available |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 41.3 mg/mL (100 mM) Ethanol: 8.3 mg/mL (20 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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