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532758 IRE1α Inhibitor, MKC-3946 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₂₀N₂O₃S

Products

Catalog NumberPackaging Qty/Pack
5.32758.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532758
Brand Family Calbiochem®
SynonymsXBP1 expression blocker, MKC3946, MKC 3946
References
ReferencesMimura, N., et al. 2012. Blood. 119, 5772.
Product Information
FormDark yellow powder
Hill FormulaC₂₁H₂₀N₂O₃S
Chemical formulaC₂₁H₂₀N₂O₃S
ReversibleY
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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°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 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.32758.0001 04055977281897

Documentation

IRE1α Inhibitor, MKC-3946 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Mimura, N., et al. 2012. Blood. 119, 5772.
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.

Revision31-July-2015 JSW
SynonymsXBP1 expression blocker, MKC3946, MKC 3946
DescriptionA cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).
FormDark yellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₁H₂₀N₂O₃S
Purity≥97% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMimura, N., et al. 2012. Blood. 119, 5772.