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412511 IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1093118-73-0C₁₅H₁₃NO₄

Products

Catalogue NumberPackaging Qty/Pack
412511-25MG Glass bottle 25 mg
Description
OverviewA cell-permeable salicylaldehyde compound that is shown to inhibit ER stress-induced Xbp1 mRNA splicing (100% inhibition by ≤25 µM in Tunicamycin-treated U373 cultures) in a reversible manner, presumably due to IRE1 inhibition via the same mechanism as 4µ8C (Cat. No. 412512) and STF083010 (Cat. No. 412510). IRE1 inhibition is shown to initiate signaling events leading to increased CRADD/RAIDD protein level (36 hrs post IRE1 inhibition in U373 cells), an important adaptor protein for caspase-2-mediated apoptosis response. Also shown to synergize with Maraba oncolytic therapy in mice (250 mg/kg/12 h via i.p. for 6 days before viral therapy) bearing Ovcar-4 or EMT6 in vivo.
Catalogue Number412511
Brand Family Calbiochem®
SynonymsER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II, 3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide
References
ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.
Product Information
CAS number1093118-73-0
FormTan solid
Hill FormulaC₁₅H₁₃NO₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetIRE1
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Use only fresh DMSO.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
412511-25MG 04055977188172

Documentation

IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem Certificates of Analysis

TitleLot Number
412511

References

Reference overview
Mahoney, D.J., et al. 2011. Cancer Cell 20, 443.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision22-November-2012 JSW
SynonymsER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II, 3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide
DescriptionA cell-permeable salicylaldehyde compound that is shown to inhibit ER stress-induced Xbp1 mRNA splicing (100% inhibition by ≤25 µM in Tunicamycin-treated U373 cultures) in a reversible manner, presumably due to IRE1 inhibition via the same molecular/chemical mechanism as 4µ8C (Cat. No. 412512) and STF083010 (Cat. No. 412510). Shown to effectively precondition/sensitize cancer cell lines (by 10,000- and 1,000-fold with 48 hrs 50 µM inhibitor pre-treatment of EMT6 and U373 cells, respectively) as well as primary cancer cultures from glioblastoma multiform patients (by ~15- to 55-fold with 48 hrs 15 µM inhibitor pre-treatment) for enhanced apoptosis upon Maraba virus infection. IRE1 inhibition is shown to initiate signaling events that eventually leads to increased CRADD/RAIDD protein level (36 hrs after initial IRE1 inhibition in U373 cells), an adaptor protein important for caspase-2-mediated apoptosis response. It is the cellular RAIDD upregulation, but not IRE1 inactivation, that is a prerequisite for the enhancing effect of rhabdovirus-mediated cancer killing. Also shown to synergize with Maraba oncolytic therapy in mice (twice daily i.p. dosing at 250 mg/kg for 6 days before viral therapy) bearing Ovcar-4 (87%, 60%, and 17% of control tumor size on day 30, respectively, with virus alone, drug alone, or combined treatment) or EMT6 (0% survival on day 20 vs. day 14, respectively, with or without combined treatment) in vivo.
FormTan solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1093118-73-0
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Use only fresh DMSO.
Toxicity Standard Handling
ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.