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CAS No. : 2377858-38-1
MCE 国际站:SCR130
产品活性:SCR130 是一种基于 SCR7 的 DNA 非同源末端连接 (NHEJ) 抑制剂。SCR130 以依赖连接酶 IV 的方式抑制 DNA 的末端连接。SCR130 对连接酶 IV 具有特异性,对连接酶 III 和连接酶 I 介导的连接的影响很小或没有影响。SCR130 诱导细胞凋亡 (apoptosis),并具有抗癌活性。
研究领域:Cell Cycle/DNA Damage | Apoptosis
作用靶点:DNA/RNA Synthesis | Apoptosis
In Vitro: SCR130 (7-21 μM; 48 hours) increase in the number of late and early apoptotic cells. SCR130 induces apoptosis by both intrinsic and extrinsic pathways. SCR130 increases the expression of p-p53, BCL2 and MCL1, and CYTOCHROME C, BAX, and BAK also increaseed. The activation of caspase 8, increase in expression of FAS and SMAC-DIABLO proteins are also observed.
SCR130 (48 hours) exhibits cytotoxicity in Reh, HeLa, CEM, Nalm6, and N114 cells with IC50 values of 14.1 μM, 5.9 μM, 6.5 μM, 2.2 μM, and 11 μM, respectively.
SCR130 can potentiate the effect of radiation (0.5 and 1 Gy) by inducing enhanced cell death upon coadministration in Reh and Nalm6 cell lines.
SCR130 blocks the endogenous NHEJ leading to accumulation of unrepaired DNA breaks. Treatment with SCR130 leads to inhibition of endogenous NHEJ, resulting in the accumulation of DNA double-strand breaks (DSBs) and cell death by activating apoptotic pathways.
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