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Mepazine

(Synonyms: 甲哌啶嗪; Pecazine) 目录号 : GC68218

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 Chemical Structure

Cas No.:60-89-9

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50mg
¥1,575.00
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100mg
¥2,295.00
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Sample solution is provided at 25 µL, 10mM.

Description

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].

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.

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.

[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.

化学性质

Cas No. 60-89-9 SDF Download SDF
别名 甲哌啶嗪; Pecazine
分子式 C19H22N2S 分子量 310.46
溶解度 DMSO : 130 mg/mL (418.73 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.221 mL 16.1051 mL 32.2103 mL
5 mM 0.6442 mL 3.221 mL 6.4421 mL
10 mM 0.3221 mL 1.6105 mL 3.221 mL
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