哌卡嗪盐酸盐

生物活性靶点体外研究体内研究哌卡嗪盐酸盐试剂级价格

哌卡嗪盐酸盐

CAS号:2975-36-2
英文名:10-[(1-methyl-3-piperidyl)methyl]-10H-phenothiazine monohydrochloride
中文名:哌卡嗪盐酸盐
CBNumber:CB3921722
分子式:C19H23ClN2S
分子量:346.91732
MOL File:2975-36-2.mol

哌卡嗪盐酸盐化学性质

熔点 :180-181 °C
沸点 :180-183 °C(Press: 0.5 Torr)
储存条件 :Store at -20°C
溶解度 :DMSO: 50 mg/mL (144.13 mM)
形态 :Solid
颜色 :White to off-white

哌卡嗪盐酸盐性质、用途与生产工艺

生物活性 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。
靶点

MALT1

体外研究

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.

Cell Viability Assay

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.

体内研究

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.

Animal Model:	6- to 8-week-old female NOD.Cg- Prkdc ^scid Il2rg ^tm1Wjl /SzJ (NSG) mice with a murine DLBCL xenogeneic tumor model
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.