1. Metabolic Enzyme/Protease NF-κB Apoptosis
  2. MALT1 Apoptosis
  3. MALT1-IN-13

MALT1-IN-13 (compound 10m) is inhibitor for mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), which to binds MALT1 protease covalently and irreversibly, inhibits MALT1 with the IC50 of 1.7 μM. MALT1-IN-13 inhibits proliferation against ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1. MALT1-IN-13 regulates mTOR and PI3K-Akt pathways.

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MALT1-IN-13

MALT1-IN-13 Chemical Structure

CAS No. : 3032823-58-5

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Description

MALT1-IN-13 (compound 10m) is inhibitor for mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), which to binds MALT1 protease covalently and irreversibly, inhibits MALT1 with the IC50 of 1.7 μM. MALT1-IN-13 inhibits proliferation against ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1. MALT1-IN-13 regulates mTOR and PI3K-Akt pathways[1].

IC50 & Target

IC50: 1.7 μM (MALT1)

Cellular Effect
Cell Line Type Value Description References
HBL1 GI50
0.69 μM
Compound: 10m
Synergistic antitumor activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs in presence of rapamycin by Cell Titer Glo assay
Synergistic antitumor activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs in presence of rapamycin by Cell Titer Glo assay
[PMID: 38349664]
HBL1 GI50
1.5 μM
Compound: 10m
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
OCI-Ly1 GI50
> 25 μM
Compound: 10m
Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
TMD8 GI50
0.7 μM
Compound: 10m
Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
In Vitro

MALT1-IN-13 (0-10 μM) induces apoptosis in HBL1 cells, inhibits proliferation against ABC-DLBCL HBL1, TMD8 and GCB-DLBCL OCI-LY1 cells with GI50 of 1.5, 0.7 and >25 μM, respecticely[1].
MALT1-IN-13 (0-10 μM) downregulates expressions of MALT1 and NF-kB pathway, upregulates the mTOR and PI3K-Akt pathway, exhibits an antitumor effect in the HBL1 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: ABC-DLBCL HBL1
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Induced over 70% apoptosis in HBL1 cells with concentration of 5 μM.

Cell Proliferation Assay[1]

Cell Line: ABC-DLBCL HBL1, ABC-DLBCL TMD8 and GCB-DLBCL OCI-LY1
Concentration: 100 μM
Incubation Time: 72 h
Result: Inhibits proliferations of ABC-DLBCL HBL1, TMD8 and GCB-DLBCL OCI-LY1.

Apoptosis Analysis[1]

Cell Line: ABC-DLBCL HBL1 and ABC-DLBCL TMD8
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased levels of cleaved PARP1 and caspase3. Decreased levels of IkBα and phosphorylated IkBα.
In Vivo

MALT1-IN-13 (25 mg/kg, i.p. for 12-14 days) exhibits an antitumor activity specific for MALT1 protease and suppresses the tumor growth in HBL1/TMD8 xenografted NCG mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HBL1/TMD8/OCI-LY1 xenografted NCG mice[1]
Dosage: 25 mg/kg
Administration: i.p., 12 days for HBL1 bearing NCG mice, 14 days for TMD8 bearing mice, 19 days for OCI-LY1 bearing mice
Result: Suppressed the HBL1 tumor growth and decreased the tumor weight with TGI of 55.9%.
Suppressed the TMD8 tumor growth and decreased the tumor weight with TGI of 69.9%.
Molecular Weight

524.84

Formula

C20H15BrClN3O3S2

CAS No.
SMILES

O=C1C(S2)=C(N=C(N1C3=CC(OC)=CC=C3OC)CBr)N(C4=CC=CC(Cl)=C4)C2=S

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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MALT1-IN-13
Cat. No.:
HY-162268
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