IRE1 Inhibitor III, 4u8C (8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde, ER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III)

Size

£386.00

SKU:: 217466
Molecular Weight:: 204.2
Purity:: ~95% (HPLC)
Storage Conditions:: -20°C
Supplier:: United States Biological
CAS Number:: 14003-96-4
Format:: Supplied as a yellow powder.
Extra Details:: A cell-permeable coumarin o-hydroxyaldehyde that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50=550 and 45nM, respectively, with 0 and 16min drug preincubation in RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50=6.9 and 4.1uM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin treatment. Comparing to STF083010, 4u8C is also shown to inhibit IRE1 autophosphorylation in cell-free assays via Schiff base formation with IRE1 Lys599 in the absence of ADP, however cellular nucleotide prevents 4u8C from targeting IRE1 Lys599 intracellularly. Formula: C11H8O4 Molecular Weight: 204.2 Solubility: DMSO (25mg/ml) Storage and Stability: Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.