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500491 MALT1 Inhibitor I, MI-2 - Calbiochem

MALT1 Inhibitor I, MI-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide, ALB-H03200218

Primary Target: MALT1
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₁₇Cl₃N₄O₃
Description
OverviewA cell-permeable chloromethyl amide that inhibits MALT1 proteolytic activity (IC50 = 5.84 µM against MALT1 paracaspase domain dimer-catalyzed Ac-LRSR-AMC hydrolysis) in an irreversible manner via covalent interaction, displaying little or no activity against caspase-3, -8, or -9. Due to irreversible binding and effective intracellular accumulation (HBL-1 intracellular [MI-2]t = 2 h = 5 µM; Medium [MI-2]t = 0 = 0.2 µM), MI-2 is at least 250-times more effective than Z-VRPR-FMK in blocking constitutive NF-κB activity and c-Rel nuclear translocation in HBL-1 cultures (equal or better blockage by 200 nM MI-2 than by 50 µM Z-VRPR-FMK). Shown to selectively inhibit MALT1-dependent ABC-DLBCL proliferation, but not the MALT1-independent growths of ABC- (HLY-1 and U2932) or GCB-DLBCL (OCI-Ly1 and OCI-Ly7) cells, both in cultures in vitro (GI50 in 48 h = 200, 400, 400, and 500 nM, respectively, against HBL-1, OCI-Ly3, OCI-Ly10, and TMD8) and in mice in vivo (65%,, 61%, and 0% suppression, respectively, of HBL-1, TMD8, and OCI-Ly1 tumor expansion 24 h after 14 daily 25 mg/kg/day i.p. dosages) without any apparent toxicity to mice.

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 Number500491
Brand Family Calbiochem®
Synonyms2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide, ALB-H03200218
References
ReferencesFontan, L., et al. 2012. Cancer Cell 22, 812.
Product Information
FormBeige solid
Hill FormulaC₁₉H₁₇Cl₃N₄O₃
Chemical formulaC₁₉H₁₇Cl₃N₄O₃
ReversibleN
Structure formula ImageStructure formula Image
Quality SegmentMQ100
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
Protect from Moisture Protect from moisture
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
Catalogue Number GTIN
500491 0

Documentation

MALT1 Inhibitor I, MI-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Fontan, L., et al. 2012. Cancer Cell 22, 812.
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.

Revision31-October-2013 JSW
Synonyms2-Chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide, ALB-H03200218
DescriptionA cell-permeable chloromethyl amide that inhibits MALT1 proteolytic activity (IC50 = 5.84 µM against MALT1 paracaspase domain dimer-catalyzed Ac-LRSR-AMC hydrolysis) in an irreversible manner via covalent interaction, displaying little or no activity against caspase-3, -8, or -9. Due to irreversible binding and effective intracellular accumulation (HBL-1 intracellular [MI-2]t = 2 h = 5 µM; Medium [MI-2]t = 0 = 0.2 µM), MI-2 is at least 250-times more effective than Z-VRPR-FMK in blocking constitutive NF-κB activity and c-Rel nuclear translocation in HBL-1 cultures (equal or better blockage by 200 nM MI-2 than by 50 µM Z-VRPR-FMK). Shown to selectively inhibit MALT1-dependent ABC-DLBCL proliferation, but not the MALT1-independent growths of ABC- (HLY-1 and U2932) or GCB-DLBCL (OCI-Ly1 and OCI-Ly7) cells, both in cultures in vitro (GI50 in 48 h = 200, 400, 400, and 500 nM, respectively, against HBL-1, OCI-Ly3, OCI-Ly10, and TMD8) and in mice in vivo (65%,, 61%, and 0% suppression, respectively, of HBL-1, TMD8, and OCI-Ly1 tumor expansion 24 h after 14 daily 25 mg/kg/day i.p. dosages) without any apparent toxicity to mice.
FormBeige solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₉H₁₇Cl₃N₄O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from moisture
Protect from light
-20°C
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
ReferencesFontan, L., et al. 2012. Cancer Cell 22, 812.