Mepazine(Synonyms: 甲哌啶嗪; Pecazine)

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Mepazine (Synonyms: 甲哌啶嗪; Pecazine)

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

Mepazine(Synonyms: 甲哌啶嗪; Pecazine)

Mepazine Chemical Structure

CAS No. : 60-89-9

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Mepazine 的其他形式现货产品:

Mepazine hydrochloride

生物活性

Mepazine (Pecazine) 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 affects viability of ABC-DLBCL cells by enhancing apoptosis[1].

IC50 & Target

MALT1[1]
体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

310.46

Formula

C19H22N2S
CAS 号

60-89-9
中文名称

甲哌啶嗪
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Nagel D, et al. Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL. Cancer Cell. 2012 Dec 11;22(6):825-37.

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