Home Immunology & Inflammation MALT inhibitor MI-2 (MALT1 inhibitor) For research use only.

MI-2 (MALT1 inhibitor)

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

MI-2 (MALT1 inhibitor) Chemical Structure

MI-2 (MALT1 inhibitor) Chemical Structure

CAS No. 1047953-91-2

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MI-2 (MALT1 inhibitor) Related Products

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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05318482 Recruiting
Cardiorespiratory Failure
Istituti Clinici Scientifici Maugeri SpA
 March 23 2022 Not Applicable

Chemical Information & Solubility

Molecular Weight 455.72 Formula

C19H17Cl3N4O3
CAS No. 1047953-91-2 SDF Download MI-2 (MALT1 inhibitor) SDF
Smiles COCCOC1=NN(C(=N1)C2=CC(=C(C=C2)Cl)Cl)C3=CC=C(C=C3)NC(=O)CCl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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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.

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