Mepazinehydrochloride(Pecazinehydrochloride)是一种有效的选择性MALT1蛋白酶抑制剂。Mepazinehydrochloride抑制全长GSTMALT1和GSTMALT1325-760段的IC50分别为0.83和0.42μM。Mepazinehydrochloride通过增强细胞凋亡(apoptosis)来影响ABC-DLBCL细胞的生存能力。
货号:ajcx31020
CAS:2975-36-2
分子式:C19H23ClN2S
分子量：346.92
溶解度:DMSO: 50 mg/mL (144.13 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Mepazine hydrochloride (Pecazine hydrochloride) 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 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)

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]

[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.