Audited Supplier
Worldyang
1597403-47-8
C22h24cl2n2o4
Pharmaceutical Intermediates
Powder
Industrial
White
659-779 Celsius Degree
2-8 Celsius Degree
≥8.96 Mg/Ml in DMSO
13.63
Worldyang
as Required
99%+
China
Product Description
Product Name: ISRIB (trans-Isomer)
CAS Number: 1597403-47-8
Appearance: White Powder
Purity: 99%
Product Description:
ISRIB (trans-isomer) is a highly selective inhibitor of PERK (PKR-like endoplasmic reticulum kinase), with an IC50 of 5 nM. It is a promising compound for research into cellular stress responses, memory enhancement, and therapeutic applications targeting unfolded protein response (UPR) pathways.
Biological Activity:
- Mechanism:
- ISRIB inhibits PERK signaling by suppressing eIF2α phosphorylation and its downstream effects, including ATF4 expression, without significantly affecting XBP1s mRNA splicing or XBP1s protein expression.
- It targets the Integrated Stress Response (ISR) by modulating translation and stress granule assembly.
- Key Metrics:
- Target: PERK (IC50 = 5 nM in a cell-free assay).
In Vitro Studies:
- ISRIB effectively inhibits endogenous ATF4 expression, reducing cellular survival rates under endoplasmic reticulum (ER) stress.
- Maintains XBP1s mRNA and protein levels, indicating selective inhibition of the PERK pathway.
In Vivo Studies:
- ISRIB exhibits favorable pharmacokinetic properties and good bioavailability in vivo.
- Animal Model: Mice injected intraperitoneally (0.25 mg/kg).
- Results:
- Enhances spatial and fear memory, improving long-term memory formation.
- Demonstrates potential in modulating cognitive functions and stress response pathways.
Applications:
- Neuroscience Research: Enhances memory and studies cellular responses to ER stress.
- Molecular Biology: Investigates the Integrated Stress Response (ISR) and unfolded protein response (UPR).
- Drug Development: Serves as a tool for developing PERK-related therapeutics.
Features:
- High Selectivity: Specifically inhibits PERK with minimal off-target effects.
- Versatile Research Uses: Applicable in memory studies, stress pathway modulation, and therapeutic development.
- Potent Activity: Demonstrates efficacy at nanomolar concentrations.
Storage Information:
- Conditions: Store at 2-8°C in a sealed container. Protect from moisture and air to maintain product stability.
Safety and Handling:
- This product is intended for research purposes only. Not for human or veterinary use.
For further inquiries regarding this product, including packaging and bulk availability, please contact us.
