SCR7吡嗪

生物活性靶点体外研究体内研究 SCR7吡嗪试剂级价格

SCR7吡嗪

CAS号:14892-97-8
英文名:"6,7-diphenyl-2-sulfanylidene-1H-pteridin-4-one
中文名:SCR7吡嗪
CBNumber:CB12741690
分子式:C18H12N4OS
分子量:332.38
MOL File:14892-97-8.mol

SCR7吡嗪化学性质

熔点 :209 °C
密度 :1.42±0.1 g/cm3(Predicted)
储存条件 :room temp
溶解度 :DMSO (Slightly), Methanol (Slightly)
酸度系数(pKa) :4.14±0.60(Predicted)
形态 :powder
颜色 :faintly yellow to dark yellow
CAS 数据库 :14892-97-8

安全信息

海关编码 :2933.59.8000

SCR7吡嗪性质、用途与生产工艺

生物活性 SCR7 pyrazine 是一种 DNA 连接酶 IV (DNA ligase IV) 抑制剂，它以连接酶 IV 依赖的方式阻断非同源末端连接 (NHEJ)。SCR7 pyrazine 也是一种 CRISPR/Cas9 的增强子，可提高 Cas9 介导的同源性定向修复 (HDR) 的效率。SCR7 pyrazine 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。
靶点

DNA Ligase IV
CRISPR/Cas9

体外研究

SCR7 pyrazine (20-100 μM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs).
SCR7 pyrazine treatment shows a dose-dependent decrease in cell proliferation with IC ₅₀ values of 40 μM, 34 μM, 44 μM, 8.5 μM, 120 μM, 10 μM and 50 μM for MCF7, A549, HeLa, T47D, A2780, HT1080 and Nalm6 cells, respectively.
In MCF7 cells, SCR7 pyrazine (20, 40 μM) treatment increases phosphorylation of ATM and activates p53, decreases MDM2, BCL2, resulting in activation of proapoptotic proteins, PUMA and BAX. And the shorter fragments of MCL1, PARP1, Caspase 3, and Caspase 9 cleavage are upregulated in a dose-dependent manner.

Western Blot Analysis

Cell Line:	MCF7 cells
Concentration:	20 μM, 40 μM, 100 μM
Incubation Time:	24 hours
Result:	Showed an increase in levels of gH2AX foci and protein.

体内研究

SCR7 pyrazine (10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan.

Animal Model:	BALB/c mice injected with breast adenocarcinoma cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; on alternate days (0, 2, 4, 6, 8, and 10)
Result:	Significantly reduced breast adenocarcinoma-induced tumor and increased lifespan.