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534330 MALT1 Inhibitor III, Mepazine Acetate - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₂₂N₂S • C₂H₄O₂

Products

Catalog NumberPackaging Qty/Pack
5.34330.0001 Glass bottle 25 mg
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
Global Trade Item Number
Catalog Number GTIN
5.34330.0001 04054839116223

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 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 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.