534330 MALT1 Inhibitor III, Mepazine Acetate - Calbiochem

534330
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₂₂N₂S • C₂H₄O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.34330.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Glass bottle 25 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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
          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.