化合物TRC 051384 T3527

Product Introduction
Bioactivity


英文名: TRC051384

描述: TRC051384 是一种热休克蛋白70 (HSP70) 诱导剂，可减少中风相关的神经元损伤并增加短暂性缺血性中风大鼠模型的存活率，激活热休克因子-1 并导致分子伴侣和抗炎活性升高，增强神经元和神经胶质细胞中 Hsp72 的表达。

细胞实验: HeLa cell transiently co-transfected with heat shock elements-luciferase reporter and normalization vector, β-galactosidase are treated with vehicle or TRC051384 (12.5 and 25 μM) for 4 hours. Cell lysates are then prepared and analyzed for luciferase and β-galactosidase activity[1].

体外活性: TRC051384 induces HSP70B mRNA by several hundred folds in both HeLa and rat primary mixed neurons in a dose-dependently manner. Treatment with TRC051384 results in a significant dose-dependent increase in HSF1 transcriptional activity and recovery of luciferase activity. TRC051384 results in 60% inhibition at 6.25 μM and 90% inhibition at 12.5 μM of LPS-induced TNF-α expression in differentiated THP-1 cell line[1].

体内活性: Treatment with TRC051384 significantly reduces stroke associated neuronal injury (87% reduction in area of penumbra recruited to infarct, and 25% reduction in brain edema) and disability in a rat model of transient ischemic stroke even though administered 8 hours post onset of ischemia. Significant improvement in survival (50% by day2 and 67.3% by day 7) is observed with TRC051384 treatment initiated at 4 hours after ischemia onset. Induction of HSP70 by TRC051384 involves HSF1 activation and results in elevated chaperone and anti-inflammatory activity[1].

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

溶解度: DMSO : 16.67 mg/mL (35.8 mM)


关键字: HSP | TRC-051384 | Heat shock proteins | Inhibitor | inhibit | TRC051384

相关产品: Novobiocin | Col003 | AMP-PCP disodium | HSP90-IN-25 | SNX0723 | AMP-PCP | HSP70-IN-1 | YUM70 | NDNA4 | H2-Gamendazole

相关库: Endoplasmic Reticulum Stress Compound Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Fibrosis Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Covalent Inhibitor Library

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