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

Mepazine (Synonyms: Pecazine)

Cat. No.: HY-121282
Handling Instructions

Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.

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Mepazine Chemical Structure

Mepazine Chemical Structure

CAS No. : 60-89-9

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Description

Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].

IC50 & Target

MALT1[1]

In Vitro

Mepazine (5-20 μM; 4 days) causes a decrease of cell viability in the activated B cell subtype of diffuse large B cell lymphoma (ABCDLBCL) cells, without significantly affecting GCB-DLBCL cells[1].

Cell Viability Assay[1]

Cell Line: ABC-DLBCL cell lines (HBL1, OCI-Ly3, U2932, TMD8, OCI-Ly10) and GCB-DLBCL cell lines (BJAB, Su-DHL-6, Su-DHL-4)
Concentration: 5, 10, and 20 μM
Incubation Time: 4 days
Result: Caused a decrease of cell viability in the ABC-DLBCL cells HBL1, OCI-Ly3, U2932, and TMD8, without significantly affecting GCB-DLBCL cells.
In Vivo

Mepazine (16 mg/kg; intraperitoneal administration) interferes with growth and induces apoptosis of ABC-DLBCL cell line OCI-Ly10 in NOD/scid IL-2Rgnull (NSG) mice with a murine DLBCL xenogeneic tumor model. Daily administration of Mepazine strongly impairs the expansion of the ABC-DLBCL cell line OCI-Ly10[1].

Animal Model: 6- to 8-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with a murine DLBCL xenogeneic tumor model[1]
Dosage: 400 μg per animal (25 g), corresponding to approximately 16 mg/kg.
Administration: Intraperitoneal administration; started 1 or 12 days after transplantation and given continuously every 24 hr; daily application
Result: Daily administration strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10.
Molecular Weight

310.46

Formula

C₁₉H₂₂N₂S

CAS No.

60-89-9

SMILES

CN1CC(CCC1)CN2C3=C(SC4=CC=CC=C24)C=CC=C3

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Keywords:

MepazinePecazineMALT1Apoptosismucosa associated lymphoid tissue lymphoma translocation gene 1diffuselargeB celllymphomaABC-DLBCLInhibitorinhibitorinhibit

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Mepazine
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