SRI-37240

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 In Vitro 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. 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). 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. SRI-37240 (10 µM; 72 h) restores CFTR function in primary bronchial epithelial cells when combination with G418. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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). IC50& Target:Premature termination codons, CFTR

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