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。

Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC 50 s 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].

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-2Rg null (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- Prkdc scid Il2rg tm1Wjl /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.

2975-36-2

C19H23ClN2S

346.92

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years