ISRIB (trans-isomer)是一种PERK的高效抑制剂，可有效逆转 eIF2α 磷酸化的作用，IC50值为 5 nM。

ISRIB (trans-isomer), the trans-isomer of ISRIB, is a effective and specific PERK inhibitor (IC50: 5 nM).

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]

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]

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].

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C22H24Cl2N2O4

451.34

ISRIB trans-isomer;trans-ISRIB;ISRIB;trans-isomer

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years