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500491 MALT1 Inhibitor I, MI-2 - Calbiochem

500491
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₁₇Cl₃N₄O₃

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      Description
      OverviewA cell-permeable chloromethyl amide that inhibits MALT1 proteolytic activity (IC50 = 5.84 µM against MALT1 paracaspase domain dimer-catalyzed Ac-LRSR-AMC hydrolysis) in an irreversible manner via covalent interaction, displaying little or no activity against caspase-3, -8, or -9. Due to irreversible binding and effective intracellular accumulation (HBL-1 intracellular [MI-2]t = 2 h = 5 µM; Medium [MI-2]t = 0 = 0.2 µM), MI-2 is at least 250-times more effective than Z-VRPR-FMK in blocking constitutive NF-κB activity and c-Rel nuclear translocation in HBL-1 cultures (equal or better blockage by 200 nM MI-2 than by 50 µM Z-VRPR-FMK). Shown to selectively inhibit MALT1-dependent ABC-DLBCL proliferation, but not the MALT1-independent growths of ABC- (HLY-1 and U2932) or GCB-DLBCL (OCI-Ly1 and OCI-Ly7) cells, both in cultures in vitro (GI50 in 48 h = 200, 400, 400, and 500 nM, respectively, against HBL-1, OCI-Ly3, OCI-Ly10, and TMD8) and in mice in vivo (65%,, 61%, and 0% suppression, respectively, of HBL-1, TMD8, and OCI-Ly1 tumor expansion 24 h after 14 daily 25 mg/kg/day i.p. dosages) without any apparent toxicity to mice.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number500491
      Brand Family Calbiochem®
      Synonyms2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide, ALB-H03200218
      References
      ReferencesFontan, L., et al. 2012. Cancer Cell 22, 812.
      Product Information
      FormBeige solid
      Hill FormulaC₁₉H₁₇Cl₃N₄O₃
      Chemical formulaC₁₉H₁₇Cl₃N₄O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMALT1
      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 -20°C
      Protect from Light Protect from light
      Protect from Moisture Protect from moisture
      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

      MALT1 Inhibitor I, MI-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Fontan, L., et al. 2012. Cancer Cell 22, 812.
      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-October-2013 JSW
      Synonyms2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide, ALB-H03200218
      DescriptionA cell-permeable chloromethyl amide that inhibits MALT1 proteolytic activity (IC50 = 5.84 µM against MALT1 paracaspase domain dimer-catalyzed Ac-LRSR-AMC hydrolysis) in an irreversible manner via covalent interaction, displaying little or no activity against caspase-3, -8, or -9. Due to irreversible binding and effective intracellular accumulation (HBL-1 intracellular [MI-2]t = 2 h = 5 µM; Medium [MI-2]t = 0 = 0.2 µM), MI-2 is at least 250-times more effective than Z-VRPR-FMK in blocking constitutive NF-κB activity and c-Rel nuclear translocation in HBL-1 cultures (equal or better blockage by 200 nM MI-2 than by 50 µM Z-VRPR-FMK). Shown to selectively inhibit MALT1-dependent ABC-DLBCL proliferation, but not the MALT1-independent growths of ABC- (HLY-1 and U2932) or GCB-DLBCL (OCI-Ly1 and OCI-Ly7) cells, both in cultures in vitro (GI50 in 48 h = 200, 400, 400, and 500 nM, respectively, against HBL-1, OCI-Ly3, OCI-Ly10, and TMD8) and in mice in vivo (65%,, 61%, and 0% suppression, respectively, of HBL-1, TMD8, and OCI-Ly1 tumor expansion 24 h after 14 daily 25 mg/kg/day i.p. dosages) without any apparent toxicity to mice.
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₁₇Cl₃N₄O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage -20°C
      Protect from moisture
      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
      ReferencesFontan, L., et al. 2012. Cancer Cell 22, 812.