SRI-37240是一种有效的提前终止密码子 (PTCs) 抑制剂。SRI-37240 抑制CFTR的无义突变。在 HEK293T 细胞中，SRI-37240 改变 PTCs 的细胞翻译终止。当与 G418 使用联合时，SRI-37240 还能恢复原发性支气管上皮细胞的 CFTR 功能。

SRI-37240 is a potent premature termination codons (PTCs) inhibitor. SRI-37240 suppresses CFTR nonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restore CFTR function in primary bronchial epithelial cells when combination with G418 [1].

SRI-37240 (1, 3, 10 and 30 μM; 48 h) induces concentration-dependent increases in CFTR-dependent ( Forskolin -stimulated and sensitive to the inhibitor CFTR Inh -172) chloride conductance [1]. SRI-37240 (10 μM; 72 h) significantly increases the amount of full-length, fully glycosylated form of CFTR protein, and the unprocessed, immature form of full-length CFTR protein in 16HBEge cells when co-treated with G418 (100 μM) [1]. SRI-37240 (10 μM; 24 h) alters cellular translation termination at PTCs in HEK293T cells, also increases global densities of ribosomes at normal stop codons without affecting densities of ribosomes in 3-UTRs [1]. SRI-37240 (10 μM; 72 h) restores CFTR function in primary bronchial epithelial cells when combination with G418 [1]. Western Blot Analysis [1] Cell Line: CFTR -G542X 16HBEge Concentration: 10 μM Incubation Time: 24 h Result: Significantly increased the amount of Band C CFTR protein, which represents the full-length, fully glycosylated form of CFTR and Band B, which represents the unprocessed, immature form of full-length CFTR protein when combined with G418 (100 μM).

883956-47-6

C24H23N3O2

385.467

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