SCR7 是一种特异性 DNA 连接酶 IV 抑制剂,可阻断非同源末端连接。它是一种不稳定的形式,可以自动循环成??稳定形式的 SCR7 pyrazine。它也是CRISPR/Cas9的增强子,可提高 Cas9 介导的同源性定向修复的效率。它诱导细胞凋亡并具有抗癌活性。
产品描述
SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).
体外活性
在负荷Dalton's淋巴瘤的Swiss albino小鼠模型中,腹腔注射SCR7(20 mg/kg)不能够消退肿瘤.在BALB/c小鼠体内,腹腔注射SCR7(20 mg/kg)能够增强辐射,依托泊苷和3-氨基苯甲酰胺对于Dalton's淋巴瘤细胞的衍生瘤的细胞毒性作用.
体内活性
在MCF7细胞(IC50=40 μM),A549细胞(IC50=34 μM),HeLa细胞(IC50=44 μM),T47D细胞(IC50=8.5 μM),A2780细胞(IC50=120 μM),HT1080细胞(IC50=10 μM),和Nalm6细胞(IC50=50 μM)中,SCR7能够显著抑制细胞增殖。
激酶实验
Complementation of SCR7 Inhibition with Puri?ed Ligase IV: Complementation experiment is carried out by adding increasing concentrations of puri?ed Ligase IV/XRCC4 complex (30, 60, and 120 fmol) along with the oligomeric DNA substrates (5' compatible and 5'-5' noncompatible ends) to the SCR7-treatedextracts. Reactions are incubated for 2 h at 25℃. The reaction products are then resolved on 8% denaturing PAGE. The gel is dried and exposed and the signal is detected with a PhosphorImager and analyzed with Multi Gauge (V3.0) software.
细胞实验
SCR7 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[3]. Wild-type, AAVS1TLR HEK293 and mouse NIH3T3 cells are maintained in DMEM supplied with 15% FBS, cells are passaged three times per week. The mouse Burkitt lymphoma cell line, generated from a Burkitt-like mouse lymphoma is maintained in DMEM supplied with 15% FBS, 2 mM HEPES, 2 mM sodium pyruvate, 2 mM L-glutamine, and 1× NAA, beta-mercaptoethanol and passaged four times per week. For puromycin selection, mCherry+ cells are sorted, seeded at 103 cells/well and selected with 3 mg/mL of Puromycin for 2 weeks. Then colonies are counted and single cells are sorted. The SCR7 inhibitor is purchased, 12 h after transfection these cells are maintained in complete medium supplied with 1 mM SCR7 inhibitor until analysis. At SCR7 concentrations of 60 mM and 10 mM, A reduction of transfection efficiency and of cell viability is observed[3].
Cas No.
1533426-72-0
分子式
C18H14N4OS
分子量
334.4
储存和溶解度
DMSO:45 mg/mL (134.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years