1449592-94-2
Chemical Structure
SMN-C5
- CAS 番号: 1449592-94-2
- Formula:C21H21FN6O
- Molecular Weight:392.44
IUPAC Name: 2-(8-fluoro-2-methylimidazo[1,2-a]pyridin-6-yl)-7-(4-methylpiperazin-1-yl)-4H-pyrido[1,2-a]pyrimidin-4-one
InChIKey: OCIABPGRNCLBEI-UHFFFAOYSA-N
SMILES: O=C1C=C(N=C2C=CC(=CN12)N3CCN(C)CC3)C=4C=C(F)C5=NC(=CN5C4)C
Biological Activity: SMN-C5 is an inducer of SMN2 exon 7 inclusion. SMN-C5 binds to the SMN2 exon 7 5′-splice site/U1 snRNA helix (Kd = 28 μM) and positively allosterically modulates SMN2 splicing correction. SMN-C5 binds to SMN2 exon 7 ESE2 and partially displaces hnRNP G, enhances the affinity of U1 snRNP for the weak splice site, binds to a bulged adenine in the major groove and forms hydrogen bonds, while not affecting the interaction of Tra2-β1 with ESE2 RNA. SMN-C5 can be used for research on spinal muscular atrophy[1][2].
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SMN-C5 | SMN-C5 is an inducer of SMN2 exon 7 inclusion. SMN-C5 binds to the SMN2 exon 7 5′-splice site/U1 snRNA helix (Kd = 28 μM) and positively allosterically modulates SMN2 splicing correction. SMN-C5 binds to SMN2 exon 7 ESE2 and partially displaces hnRNP G, enhances the affinity of U1 snRNP for the weak splice site, binds to a bulged adenine in the major groove and forms hydrogen bonds, while not affecting the interaction of Tra2-β1 with ESE2 RNA. SMN-C5 can be used for research on spinal muscular atrophy. | |||||||||||||||||||||
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References
- [1]. Sivaramakrishnan M, et al. Binding to SMN2 pre-mRNA-protein complex elicits specificity for small molecule splicing modifiers. Nature communications. 2017 Nov 14;8(1):1476.
- [2]. Malard F, et al. The diversity of splicing modifiers acting on A-1 bulged 5'-splice sites reveals rules for rational drug design. Nucleic acids research. 2024 May 08;52(8):4124-4136.
