Bioactivity | 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]. | ||||||||||||
Target | Premature termination codons, CFTR | ||||||||||||
Invitro | SRI-37240 (1, 3, 10 and 30 µM; 48 h) induces concentration-dependent increases in CFTR-dependent (Forskolin-stimulated and sensitive to the inhibitor CFTRInh-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: | ||||||||||||
Name | SRI-37240 | ||||||||||||
CAS | 883956-47-6 | ||||||||||||
Formula | C24H23N3O2 | ||||||||||||
Molar Mass | 385.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Sharma J, et al. A small molecule that induces translational readthrough of CFTR nonsense mutations by eRF1 depletion. Nat Commun. 2021 Jul 16;12(1):4358. |