500500 MALT1 Inhibitor II, Mepazine Hydrochloride - CAS 2975-36-2 - Calbiochem

500500
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₉H₂₃ClN₂S2975-36-2

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      5.00500.0001
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          Glass bottle 25 mg
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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.
          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 number2975-36-2
          FormGreyish to off-white powder
          FormulationSupplied as a hydrochloride salt.
          Hill FormulaC₁₉H₂₃ClN₂S
          Chemical formulaC₁₉H₂₃ClN₂S
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Schlauderer, F., et al. 2013. Angew. Chem. Int. Ed. 52, In press.
          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.

          Revision10-May-2013 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.
          FormGreyish to off-white powder
          FormulationSupplied as a hydrochloride salt.
          Intert gas (Yes/No) Packaged under inert gas
          CAS number2975-36-2
          Chemical formulaC₁₉H₂₃ClN₂S
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (25 mg/ml) or H₂O (2.5 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 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.