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Product Details

4μ8C | IRE1 ribonuclease inhibitor

4μ8C (14003-96-4) is a selective inhibitor of IRE1α ribonuclease (RNase) activity (IC50 = 60 nM). Covalently binds to lysine 907 in the IRE1 endonuclease domain, blocking substrate access to the active site of IRE1α and inactivating both XBP1 splicing and IRE1α-mediated mRNA degradation but not IRE1 kinase activity.1 Inhibits IRE1α in response to hypoxia or other ER stress-inducing agents but has no effect on proliferation or clonogenic survival of hypoxic cells.2 Blocks production of IL-4, IL-5 and IL-13 production in T cells.3 4μ8C prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production in pancreatic β-cells.4

References/Citations

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 IRE1α 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 1α (IRE1α) 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 β-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis;  BMC Cell Biol., 15 29

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Focus Biomolecules cell signaling reagent supplier, chemical structure 4μ8C | IRE1 ribonuclease inhibitor | CAS 14003-96-4

Catalog#  10-1579

$75.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
14003-96-4
Catalog Number:
10-1579
Activity:
IRE1 ribonuclease inhibitor
Chemical Name:
7-Hydroxy-4-methyl-2-oxo-2H-1-benzopyran-8-carboxaldehyde
Molecular Weight:
204.18
Molecular Formula:
C11H8O4
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
Yellow solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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