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534330 MALT1 Inhibitor III, Mepazine Acetate - Calbiochem

534330
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₂₂N₂S • C₂H₄O₂

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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable phenothiazine that inhibits MALT1, but not caspase-3 or -8, proteolytic activity (IC50 = 0.83 and 0.42 µM, respectively, against full-length or paracaspase domain-containing aa 325-760 MALT1 GST fusion-catalyzed Ac-LRSR-AMC hydrolysis) in a reversible and noncompetitive manner and blocks anti-CD3/CD28-stimulated IL-6 production (20 h) in primary murine CD4+ T-cell (by 77%) and human PBMC cultures (by 51 - 89%). Shown to suppress ABC-DLBCL constitutive cellular MALT1 activity (>75% suppression by 10 µM Mepazine; IC50 <5 µM in U2932, OCI-Ly10, OCI-Ly3, HBL1, and TMD8 cultures) and RelB cleavage, resulting in effective blockage of NF-κB-dependent IL-6, IL-10, as well as anti-apoptotic Bcl-xL and FLIP-L expressions. Mepazine exhibits ABC-DLBCL-selective cytotoxicity (≥27% cell death in 4 days by 10 µM Mepazine in HBL-1, OCI-Ly3, OCI-Ly10, TMD8, and U2932 cultures) over GCB-DLBCL (≤26% cell death in 4 days by 20 µM Mepazine in DJAB, Su-DHL-4, and Su-DHL-6 cultures) both in cultures in vitro and in mice (74%, and 0% suppression, respectively, of OCI-Ly10 and Su-DHL-6 tumor expansion on day 22 post cancer transplant; via daily 400 µg/kg i.p.) in vivo.
      Catalogue Number534330
      Brand Family Calbiochem®
      SynonymsPacatal, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Acetate, Mucosa-Associated Lymphoid tissue Lymphoma Translocation 1 Inhibitor III, MALT-1 Inhibitor III
      References
      ReferencesSchlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, 10384.
      Nagel, D., et al. 2012. Cancer Cell. 22, 825.
      Product Information
      FormPurple solid
      Hill FormulaC₁₉H₂₂N₂S • C₂H₄O₂
      Chemical formulaC₁₉H₂₂N₂S • C₂H₄O₂
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMALT1
      Primary Target IC<sub>50</sub>0.83 and 0.42 µ
      Purity≥95% 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
      Hygroscopic Hygroscopic
      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 III, Mepazine Acetate - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Schlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, 10384.
      Nagel, D., et al. 2012. Cancer Cell. 22, 825.
      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.

      Revision08-September-2017 JSW
      SynonymsPacatal, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Acetate, Mucosa-Associated Lymphoid tissue Lymphoma Translocation 1 Inhibitor III, MALT-1 Inhibitor III
      DescriptionA cell-permeable phenothiazine that inhibits MALT1, but not caspase-3 or -8, proteolytic activity (IC50 = 0.83 and 0.42 µM, respectively, against full-length or paracaspase domain-containing aa 325-760 MALT1 GST fusion-catalyzed Ac-LRSR-AMC hydrolysis) in a reversible and noncompetitive manner and blocks anti-CD3/CD28-stimulated IL-6 production (20 h) in primary murine CD4+ T-cell (by 77%) and human PBMC cultures (by 51 - 89%). Shown to suppress ABC-DLBCL constitutive cellular MALT1 activity (>75% suppression by 10 µM Mepazine; IC50 <5 µM in U2932, OCI-Ly10, OCI-Ly3, HBL1, and TMD8 cultures) and RelB cleavage, resulting in effective blockage of NF-κB-dependent IL-6, IL-10, as well as anti-apoptotic Bcl-xL and FLIP-L expressions. Mepazine exhibits ABC-DLBCL-selective cytotoxicity (≥27% cell death in 4 days by 10 µM Mepazine in HBL-1, OCI-Ly3, OCI-Ly10, TMD8, and U2932 cultures) over GCB-DLBCL (≤26% cell death in 4 days by 20 µM Mepazine in DJAB, Su-DHL-4, and Su-DHL-6 cultures) both in cultures in vitro and in mice (74%, and 0% suppression, respectively, of OCI-Ly10 and Su-DHL-6 tumor expansion on day 22 post cancer transplant; via daily 400 µg/kg i.p.) in vivo.
      FormPurple solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₂₂N₂S • C₂H₄O₂
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (50 mg/ml)
      Storage -20°C
      Hygroscopic
      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
      ReferencesSchlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, 10384.
      Nagel, D., et al. 2012. Cancer Cell. 22, 825.