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

Mepazine hydrochloride (Synonyms: Pecazine hydrochloride)

目录号: HY-121282A
产品使用指南

Mepazine hydrochloride (Pecazine hydrochloride) 是一种有效的选择性 MALT1 蛋白酶抑制剂。Mepazine hydrochloride 抑制全长 GSTMALT1 和 GSTMALT1 325-760 段的IC50 分别为 0.83 和 0.42 μM。Mepazine hydrochloride 通过增强细胞凋亡 (apoptosis) 来影响 ABC-DLBCL 细胞的生存能力。

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Mepazine hydrochloride Chemical Structure

Mepazine hydrochloride Chemical Structure

CAS No. : 2975-36-2

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Description

Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride 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

346.92

Formula

C₁₉H₂₃ClN₂S

CAS No.

2975-36-2

中文名称

甲哌啶嗪盐酸盐

SMILES

CN1CC(CN2C3=C(C=CC=C3)SC4=CC=CC=C24)CCC1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

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

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Mepazine hydrochloride
目录号:
HY-121282A
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