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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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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Overview

Replacement Information

Key Spec Table

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

Products

Catalogue NumberPackaging Qty/Pack
5.00500.0001 Glass bottle 25 mg
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
Catalogue Number GTIN
5.00500.0001 04055977245646

Documentation

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

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.