Mepazine
(Synonyms: 甲哌啶嗪; Pecazine) 目录号 : GC68218Mepazine (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。
Cas No.:60-89-9
Sample solution is provided at 25 µL, 10mM.
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.
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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