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Cat. No.: HY-162268

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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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CAS No.: 3032823-58-5
Formule: C₂₀H₁₅BrClN₃O₃S₂
Masse moléculaire:524.84

Stockage:

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

Data Sheet (276 KB)

MALT1-IN-13 Chemical Structure

CAS No.: 3032823-58-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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%.

Chemical Information

CAS No. 3032823-58-5
Masse moléculaire 524.84
Formule C₂₀H₁₅BrClN₃O₃S₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Liang X, et al., Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma. J Med Chem. 2024 Feb 22;67(4):2884-2906.

[2]. Liang X, et al., Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma. J Med Chem. 2024 Feb 22;67(4):2884-2906. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

MOQ

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100 mg

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