| Bioactivity | UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides[1]. | ||||||||||||
| Invitro | UNC10217938A strongly enhances luciferase induction in HelaLuc705 cells when used in the 5-25 µM range and are substantially more effective and potent than Retro-1. As compared to splice switching oligonucleotide (SSO) alone, UNC10217938A provids a 60-fold enhancement at 10 µM and 220-fold at 20 µM, in contrast to a 11-fold enhancement for 100 µM Retro-1[1].UNC10217938A can substantially enhance effects of receptor targeted oligonucleotide conjugates. UNC10217938A also can enhance effects of uncharged morpholino oligonucleotides as well as negatively charged oligonucleotides[1].Exposure of cells to UNC10217938A leads to a major reduction in co-localization of the TAMRA-oliogonucleotide with the late endosome marker Rab7, but had little effect on co-localization with the lysosomal marker LAMP-1. UNC10217938A causes partial release of oligonucleotide from late endosomes to the cytosol followed by nuclear accumulation[1]. | ||||||||||||
| In Vivo | Systemic treatment with SSO623 followed by administration of UNC10217938A (7.5 mg/kg; intravenous injection) produces distinct increases in EGFP fluorescence in liver, kidney and heart in EGFP654 mice[3]. | ||||||||||||
| Name | UNC10217938A | ||||||||||||
| CAS | 1347749-97-6 | ||||||||||||
| Formula | C26H28N6O2 | ||||||||||||
| Molar Mass | 456.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Yang B, et al. High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides. Nucleic Acids Res. 2015 Feb 27;43(4):1987-96. |
UNC10217938A
CAS: 1347749-97-6 F: C26H28N6O2 W: 456.54
UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucl
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