MI-2 (MALT1 inhibitor)

Catalog No.S7429

For research use only.

MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor with IC50 of 5.84 μM.

MI-2 (MALT1 inhibitor) Chemical Structure

CAS No. 1047953-91-2

Selleck's MI-2 (MALT1 inhibitor) has been cited by 8 Publications

1 Customer Review

Purity & Quality Control

Choose Selective MALT Inhibitors

Biological Activity

Description MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor with IC50 of 5.84 μM.
Targets
MALT1 [1]
(cell-free assay)
5.84 μM
In vitro

MI-2 inhibits MALT1 functions in ABC-DLBCL cell lines with excellent cell penetration. MI-2 produces selective growth inhibition for MALT1-dependent cell lines with GI50 of 0.2, 0.5, 0.4, and 0.4 礛 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, whereas the ABC-DLBCL MALT1-independent cell lines, U2932 and HLY-1, and the two GCB-DLBCL cell lines were resistant. [1]

In vivo MI-2 (350 mg/kg) is nontoxic to mice. MI-2 (25 mg/kg/day i.p.) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts, whereas it has no effect on the growth of OCI-Ly1 tumors. [1]

Protocol (from reference)

Kinase Assay:[1]
  • High-Throughput Screening for MALT1 Proteolytic Activity Inhibitors:

    Ac-LRSR-AMC is used as substrate and reactions are measured with excitation/emission wavelengths of 360/465 nm. Two time points are measured for each reaction to eliminate false positives due to compound autofluorescence. The final percent inhibition is calculated with the formula {[fluorescencetest compound (T2-T1)-fluorescenceneg ctrl (T2-T1)]/[fluorescencepos ctrl (T2-T1)-fluorescenceneg ctrl (T2-T1)]} × 100, where Z-VRPR-FMK (300 nM) is used as positive control and buffer only as negative control. The positive hits are validated in concentration-response experiments within a dose range of 0.122–62.5 µM to determine IC50 of the compounds. Activity is validated using recombinant full-length wild-type MALT1.

Cell Research:[1]
  • Cell lines: MALT1-independent cell lines: U2932 and HLY-1, and the two GCB-DLBCL cell lines; MALT1-dependent cell lines: HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells.
  • Concentrations: ~5 μM
  • Incubation Time: 48 hours
  • Method: Cell proliferation is determined by ATP quantification using a luminescent method and trypan blue dye exclusion. Standard curves for each cell line are calculated by plotting the cell number (determined using trypan blue) against their luminescence values, and cell number is calculated accordingly. Cell viability in drug-treated cells is normalized to their respective controls (fractional viability), and results are given as 1-fractional viability. CompuSyn software is used to determine GI25 and GI50 values.
Animal Research:[1]
  • Animal Models: SCID NOD.CB17-Prkdcscid/J mice bearing human HBL-1, TMD8, or OCI-Ly1 xenograft.
  • Dosages: 25 mg/kg/day
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 91 mg/mL
(199.68 mM)
Ethanol 91 mg/mL
(199.68 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+30%PEG300+5%Tween-80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 455.72
Formula

C19H17Cl3N4O3

CAS No. 1047953-91-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COCCOC1=NN(C(=N1)C2=CC(=C(C=C2)Cl)Cl)C3=CC=C(C=C3)NC(=O)CCl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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