ISRIB (trans-isomer)

SKU: orb1301002

Description

ISRIB (trans-isomer)

Research Area

Cell Biology

Key Properties

• CAS Number: 1597403-47-8
• MW: 451.34
• Purity: 98.81%
• Formula: C₂₂H₂₄Cl₂N₂O₄
• SMILES: Clc1ccc(OCC(=O)N[C@H]2CC[C@@H](CC2)NC(=O)COc2ccc(Cl)cc2)cc1
• Target: Autophagy,PERK,Apoptosis
• Solubility: DMSO:1.11 mg/mL (2.46 mM);10% DMSO+90% Saline:0.11 mg/mL (0.24 mM)

Bioactivity

• Target IC50:
  PERK:5 nM
• In Vivo:
  METHODS: To investigat the effects on memory, ISRIB (0.25-2.5 mg/kg) was administered intraperitoneally to CD-1 mice. Results: ISRIB-treated mice showed significant enhancement in spatial and fear-related learning.
• In Vitro:
  METHODS: HEK293T cells were treated with clindamycin (2 µg/mL) to induce ER stress and with ISRIB (trans-isomer) or ISRIB (cis-isomer) (0-1 µM) for 7 h the ATF4 fluorokinase Reporter gene was detected. Results: ISRIB (trans-isomer) was 100-fold more potent IC50 5 nM) than ISRIB (cis-isomer) IC50 600 nM), suggesting tha the compound interacts stereospecifically with its cellular target. METHODS: HEK293T cells were treated with Tm (1 µg/mL) and ISRIB (200 nM) for 1 h. Translation and mRNA Changes were detected. Results: ISRIB completely blocke the translational Changes that occurred under ER stress. A large number of genes with significant Changes in expression upon stress collapsed to the center o the graph under ISRIB and Tm co-treatment.
• Cell Research:
  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 fo the indicated an the level of eIF2α phosphorylation is determine.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

PKR-like endoplasmic reticulum kinase, PERK, Protein kinase R-like endoplasmic reticulum kinase, Autophagy, Apoptosis, ISRIB (trans isomer), ISRIB (transisomer), ISRIB (trans-isomer), ISRIB trans-isomer

Compound Identifiers

PubChem CID

1011240