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。
生物活性 | Mepazine (Pecazine) is a potent and selectiveMALT1protease inhibitor withIC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancingapoptosis[1]. |
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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].
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. |
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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].
Animal Model: | 6- to 8-week-old female NOD.Cg-PrkdcscidIl2rgtm1Wjl/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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Pure form | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(322.10 mM;Need ultrasonic) 配制储备液 1 mM | 3.2210 mL | 16.1051 mL | 32.2103 mL | 5 mM | 0.6442 mL | 3.2210 mL | 6.4421 mL | 10 mM | 0.3221 mL | 1.6105 mL | 3.2210 mL |
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