sirna modification

1. Chemically-Modified siRNA siRNA is one of the valued tools which is widely used to investigate the functions of genes and gene silencing. However, poor stability, immunogenic and off-target effects make siRNA is not optimal drug-like molecule. Chemically-modified siRNA overcomes these challenges, chemical modifications of siRNA therapeutics significantly improve their pharmacological and therapeutic properties. There are three kinds of chemical modifications Ribose modification Ribose modification can strongly influence sugar conformation as it allows the oligonucleotide to adopt the energetically favorable conformation, therefore, formation of thermally stable A-type duplexes was expected upon the introduction of these modifications into siRNAs. And ribose modifications can also improve endonuclease resistance. Examples: 2′-O-Me, 2′-O-methoxyethyl (2′-O-MOE), 2 -O-allyl, 2 -O-cyanoethyl), 2 -O-ethylamine, 2 -O-DNP, 2 F-RNA, 2 F-ANA, 4 S-RNA and 4 S-2 F-ANA). Phosphate backbone modification Chemical modifications to the phosphate backbone are tolerated by RNAi. Internucleotide linkages used in siRNA will retain the negative charge of a phosphate and can be cleaved by endo and exonucleases. Examples: phosphorothioate linkage, boranophosphate linkage, phosphonoacetate linkage. Base modification The use of base modification is more limited than other kinds of chemical modifications, but there are still many applications. Some modified bases can stabilize AU base pairs and increase the strength of AU base pairs. Examples: 5-halouracils, 2- thiouracil, pseudouracil, diaminopurine. BOC RNA provides high-quality and cost-effective siRNA with various chemical modifications and flexible synthesis scales to meet customers' needs.

2. All our chemically-modified siRNAs are purified by HPLC, and supplied in lyophilized powder. The quantity we can provide ranges from 2 OD to 250 OD. Cat No. Modification Quantity Purification Price Lead Time BRD-001 Deoxyinosine 2 OD-250 OD HPLC Inquiry Inquiry BRD-002 2'-Fluoro-rU 2 OD-250 OD HPLC Inquiry Inquiry BRD-003 2'-Fluoro-rC 2 OD-250 OD HPLC Inquiry Inquiry BRD-004 5'-Bromo-rU 2 OD-250 OD HPLC Inquiry Inquiry BRD-005 2'-OMe-rU 2 OD-250 OD HPLC Inquiry Inquiry BRD-006 2'-OMe-rC 2 OD-250 OD HPLC Inquiry Inquiry BRD-007 2'-OMe-rG 2 OD-250 OD HPLC Inquiry Inquiry BRD-008 2'-OMe-rA 2 OD-250 OD HPLC Inquiry Inquiry BRD-009 5'-Phosphate 2 OD-250 OD HPLC Inquiry Inquiry BRD-010 3'-Phosphate 2 OD-250 OD HPLC Inquiry Inquiry BRD-011 5'-Amine 2 OD-250 OD HPLC Inquiry Inquiry BRD-012 3'-Amine 2 OD-250 OD HPLC Inquiry Inquiry BRD-013 5'-Biotin 2 OD-250 OD HPLC Inquiry Inquiry

3. BRD-014 3'-Biotin 2 OD-250 OD HPLC Inquiry Inquiry BRD-015 5'-Thiol 2 OD-250 OD HPLC Inquiry Inquiry BRD-016 3'-Thiol 2 OD-250 OD HPLC Inquiry Inquiry BRD-017 5'-Digoxin 2 OD-250 OD HPLC Inquiry Inquiry BRD-018 3'-Digoxin 2 OD-250 OD HPLC Inquiry Inquiry BRD-019 Spacer C3 2 OD-250 OD HPLC Inquiry Inquiry BRD-020 Spacer C6 2 OD-250 OD HPLC Inquiry Inquiry BRD-021 Spacer 9 2 OD-250 OD HPLC Inquiry Inquiry BRD-022 Spacer 18 2 OD-250 OD HPLC Inquiry Inquiry BRD-023 5'-Cholesterol 2 OD-250 OD HPLC Inquiry Inquiry BRD-024 5'-Ferrocene 2 OD-250 OD HPLC Inquiry Inquiry BRD-025 3'-Ferrocene 2 OD-250 OD HPLC Inquiry Inquiry BRD-026 2'-Isoproply 2 OD-250 OD HPLC Inquiry Inquiry BRD-027 phosphorothioates 2 OD-250 OD HPLC Inquiry Inquiry Please send email to rna@bocsci.com if you need other modifications. Order Request

4. Ref: 1.WATTS, J., DELEAVEY, G., & DAMHA, M. (2008). Chemically modified siRNA: tools and applications. Drug Discovery Today, 13(19-20), 842–855. 2.Selvam, C., Mutisya, D., Prakash, S., Ranganna, K., & Thilagavathi, R. (2017). Therapeutic potential of chemically modified siRNA: Recent trends. Chemical Biology & Drug Design, 90(5), 665–678. 3.Deleavey, G. F., Watts, J. K., & Damha, M. J. (2009). Chemical Modification of siRNA. Current Protocols in Nucleic Acid Chemistry, 16.3.1–16.3.22. Related Products Labels Phosphoramidites https://rna.bocsci.com/products-services/chemically-modified-sirna.html