ISRIB (trans-isomer)
作者：齐岳
发布时间：2023-09-13
17:03:52
点击数：
产品名称：ISRIB (trans-isomer)
产品描述：
| 产品描述 | ISRIB (trans-isomer), the trans-isomer of ISRIB, is a effective and specific PERK inhibitor (IC50: 5 nM). |
| 靶点活性 | PERK:5 nM |
| 体外活性 | ISRIB blocks production of endogenous ATF4, whereas XBP1 mRNA splicing and XBP1s production persisted. ISRIB prevents cells from re-establishing ER homeostasis by blocking signaling through the PERK branch of the UPR, and decreases the viability of cells that are subjected to ER-stress. [1] |
| 体内活性 | ISRIB shows favorable properties in pharmacokinetic profiling experiments and good bioavailability in vivo. ISRIB (0.25 mg/kg i.p.) increases long-term memory in mice by enhancing spatial and fear-associated learning. [1] |
| 细胞实验 | U2OS cells are plated on 96-well plates and left to recover overnight. Cells are treated with either with 2 μg/ml tunicamycin or 100 nM thapsigargin in the presence or absence of 100 nM ISRIB or with ISRIB alone for the indicated and the level of eIF2α phosphorylation is determined[1]. |
| 别名 | trans-isomer, ISRIB, ISRIB trans-isomer, trans-ISRIB |
| 分子量 | 451.34 |
| 分子式 | C22H24Cl2N2O4 |
| CAS No. | 1597403-47-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: <4.51mg（10.00mM）
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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