Description
- SKU:
- 10-1579-25mg
- CAS Number:
- 14003-96-4
- Extra Details:
- Selective inhibitor of IRE1? ribonuclease (RNase) activity (IC50 = 60 nM). Covalently binds to lysine 907 in the IRE1 endonuclease domain, blocking substrate access to the active site of IRE1? and inactivating both XBP1 splicing and IRE1?-mediated mRNA degradation but not IRE1 kinase activity1. Inhibits IRE1? in response to hypoxia or other ER stress-inducing agents but has no effect on proliferation or clonogenic survival of hypoxic cells2. Blocks production of IL-4, IL-5 and IL-13 production in T cells3. Prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production in pancreatic ?-cells4.
- Molecular Weight:
- 204.18
- Physical State:
- Yellow solid
- References:
- 1) Cross et al. (2012), The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule; Proc. Natl. Acad. Sci. USA., 109 E869 2) Cojocari et al. (2013), New small molecule inhibitors of UPR activation demonstrate that PERK, but not IRE1? signaling is essential for promoting adaptation and survival to hypoxia; Radiother. Oncol., 108 541 3) Kemp et al. (2013), The serine-threonine kinase inositol-requiring enzyme 1? (IRE1?) promotes IL-4 production in T helper cells; J. Biol. Chem., 288 33272 4) Zhang et al. (2014), IRE1 inhibition perturbs the unfolded protein response in a pancreatic ?-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis; BMC Cell Biol., 15 29
- Shipping Conditions:
- Ambient
- Storage Conditions:
- -20°C
- Supplier:
- Focus Biomolecules
- Purity:
- 97% by TLC NMR (Conforms)
- Chemical Name:
- 7-Hydroxy-4-methyl-2-oxo-2H-1-benzopyran-8-carboxaldehyde
