532758 IRE1α Inhibitor, MKC-3946 - Calbiochem

532758
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₂₀N₂O₃S

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      Glass bottle 10 mg
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      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

      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 -20°C
      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.
      Toxicity Standard Handling
      ReferencesMimura, N., et al. 2012. Blood. 119, 5772.