4-吡啶羧酸 2-苯基酰肼 T1869

Product Introduction
Bioactivity


英文名: PluriSIn 1

描述: PluriSIn 1 (NSC 14613) 是一种酰基-辅酶 A 去饱和酶抑制剂，是一种多能细胞特异性的抑制剂。

细胞实验: Relative cell numbers are determined by fixating the cells with 0.5% glutardialdehyde and staining with methylene blue dissolved in 0.1 M boric acid (pH 8.5). Color extraction is performed using 0.1 M hydrochloric acid, and the staining (which is proportional to cell number) is quantitated by measuring absorbance at 650 nM.(Only for Reference)

激酶实验: SCD1 activity assays: Cells are plated in 6-well plates at a density of 50k to 100k cells per well. 24 h later, 20 μM PluriSIn #1 or 0.2% DMSO-control are added to the cells. After 12 h of incubation at 37 ℃, 5% CO2, the old medium is removed, cells are washed with PBS, and new medium containing 2.3 μM of 0.75 UCi [1-14C] Stearic Acid is added. The cells are incubated for up to 4 h at 37 ℃, 5% CO2. After the incubation period, the medium is discarded and the cells are washed 3 times with 2 mL of PBS. 2 mL of the mixture n-hexane: isopropanol (3:2 v:v) are added, and the cells are incubated for 30 min at 37 ℃, 5% CO2. 2 mL Folch solution (chloroform: methanol,2:1,v:v) are subsequently added. The liquid is transferred to tubes for phase partition by adding 1 mL water. The lower organic phase is evaporated and used for lipid saponification and TLC separation of the free [1-14C] Stearic Acid (substrate) and [1-14C] Oleic Acid (formed product). Lipids extracted from the cells are applied to TLC plates previously immersed in 10% NO3 Ag and activated at 120℃x60 min. Unlabeled stearic and oleic acid are added to each application point as carriers and as internal standards for identification. The plates are run with a solvent mixture of Chloroform:MeOH:AcH:DDW (90:8:1:0.8). The free fatty acids are detected by U.V. after spraying the TLC with a 2',7',dichlorofluorescein solution. The spots corresponding to stearic and oleic acid are scraped and the radioactivity counted in a sc intillating counter. SCD1 desaturase activity is calculated from the percent conversion of substrate to product and the conversion to pmol/min/106 cells.

体内活性: PluriSIn 1通过激活细胞凋亡使中央细胞死亡。PluriSIn 1通过与hPSCs的作用产生ER应激。PluriSIns 1（20 μM）对未分化hPSCs形成畸胎瘤的过程具有抑制作用,其还抑制mPSCs和小鼠胚胎发育。PluriSIns 1（20 μM）通过与hPSCs作用诱导蛋白质合成降低约30%。作用于hPSCs时,PluriSIns 1可产生强效快速且具有选择性的细胞毒性,还可诱导硬脂酰辅酶A脱氢酶活性降低~65%。

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

溶解度: DMSO : 21.3 mg/mL (100 mM)
Ethanol : 21.3 mg/mL (100 mM)


关键字: Apoptosis | Stearoyl-CoA Desaturase (SCD) | PluriSIn-1 | NSC14613 | Inhibitor | PluriSIn1 | inhibit | PluriSIn 1 | NSC-14613

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相关库: Anti-Aging Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Lipid Metabolism Compound Library | Apoptosis Compound Library | Metabolism Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library

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