化合物SW033291 T2121

Product Introduction
Bioactivity


英文名: SW033291

描述: 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。

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).

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: In mice receiving a bone marrow transplant, SW033291 (10 mg/kg, i.p.) promotes hematopoietic recovery. In mouse models of colon and liver injury, SW033291 (10 mg/kg, i.p.) reduces the levels of colitis-associated inflammatory cytokines, protects mice from colitis, and promotes liver regeneration. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 41.3 mg/mL (100 mM)
Ethanol : 8.3 mg/mL (20 mM)


关键字: knockout | PGE2 | 15-PGDH | Peripheral | prostaglandin | bone | SW033291 | inhibit | neutrophil | SW-033291 | SW 033291 | hematopoietic | 15-Hydroxyprostaglandin dehydrogenase | marrow | Inhibitor

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相关库: Anti-Cancer Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途