SRI-37240

• CAT Number: I042870
• CAS Number: 883956-47-6
• Molecular Formula: C24H23N3O2
• Molecular Weight: 385.46
• Purity: ≥95%
• Synonyms: 3-cyclohexyl-10-methyl-2-phenylpyrimido[4,5-b]quinoline-4,5-dione
• InChI: InChI=1S/C24H23N3O2/c1-26-19-15-9-8-14-18(19)21(28)20-23(26)25-22(16-10-4-2-5-11-16)27(24(20)29)17-12-6-3-7-13-17/h2,4-5,8-11,14-15,17H,3,6-7,12-13H2,1H3
• InChIKey: VMNOIZKDWKJSPW-UHFFFAOYSA-N
• SMILES: CN1C2=CC=CC=C2C(=O)C3=C1N=C(N(C3=O)C4CCCCC4)C5=CC=CC=C5

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 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].

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.
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