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500500 MALT1 Inhibitor II, Mepazine Hydrochloride - CAS 738596-90-2 - Calbiochem

MALT1 Inhibitor II, Mepazine HCl, CAS 738596-90-2, is a cell-permeable inhibitor of MALT1. Does not affect caspase-3 or -8 activities.

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Synonymes: MALT-1 Inhibitor II, Mucosa-Associated Lymphoid tissue Lymphoma Translocation 1 Inhibitor II, Pacatal, 10-((1-Methylpiperidin-3-yl)methyl)-10H-phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidyl)methyl)phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Hydrochloride

Primary Target: MALT1
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500500
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Tableau de caractéristiques principal

CAS #Empirical Formula
738596-90-2C₁₉H₂₃ClN₂S • x HCl

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      Description
      OverviewA cell-permeable phenothiazine that 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-catalyzed Ac-LRSR-AMC hydrolysis) in a reversible and noncompetitive manner. Shown to suppress ABC-DLBCL constitutive cellular MALT1 activity (by >75% at 10 µM; IC50 <5 µM in U2932, OCI-Ly10, OCI-Ly3, HBL1, and TMD8 cultures) and RelB cleavage, resulting in ABC-DLBCL-selective cytotoxicity (≥27% cell death in 4 days at 10 µM) over GCB-DLBCL (≤26% cell death in 4 days at 20 µM) both in cultures in vitro and in mice (400 µg/kg daily i.p.) in vivo.

      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. In addition, the CAS number provided represents variable hydrochloride content; the parent compound CAS number is 60-89-9 and the monohydrochloride CAS number is 2975-36-2.
      Catalogue Number500500
      Brand Family Calbiochem®
      SynonymsMALT-1 Inhibitor II, Mucosa-Associated Lymphoid tissue Lymphoma Translocation 1 Inhibitor II, Pacatal, 10-((1-Methylpiperidin-3-yl)methyl)-10H-phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidyl)methyl)phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Hydrochloride
      References
      ReferencesSchlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, In press.
      Nagel, D., et al. 2012. Cancer Cell 22, 825.
      Product Information
      CAS number738596-90-2
      FormGreyish to off-white powder
      FormulationSupplied as a hydrochloride salt.
      Hill FormulaC₁₉H₂₃ClN₂S • x HCl
      Chemical formulaC₁₉H₂₃ClN₂S • x HCl
      Hygroscopic Hygroscopic
      ReversibleY
      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
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5005000001 04055977245646

      Documentation

      MALT1 Inhibitor II, Mepazine Hydrochloride - CAS 738596-90-2 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Schlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, In press.
      Nagel, D., et al. 2012. Cancer Cell 22, 825.
      Fiche technique

      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.

      Revision28-August-2019 JSW
      SynonymsMALT-1 Inhibitor II, Mucosa-Associated Lymphoid tissue Lymphoma Translocation 1 Inhibitor II, Pacatal, 10-((1-Methylpiperidin-3-yl)methyl)-10H-phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidyl)methyl)phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Hydrochloride
      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.

      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. In addition, the CAS number provided represents variable hydrochloride content; the parent compound CAS number is 60-89-9 and the monohydrochloride CAS number is 2975-36-2.
      FormGreyish to off-white powder
      FormulationSupplied as a hydrochloride salt.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number738596-90-2
      Chemical formulaC₁₉H₂₃ClN₂S • x HCl
      Purity≥97% by HPLC
      SolubilityDMSO (25 mg/ml) or H₂O (2.5 mg/ml)
      Storage Protect from light
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesSchlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, In press.
      Nagel, D., et al. 2012. Cancer Cell 22, 825.