1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. ODN 2216 sodium

ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4+ T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4+ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8+ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus.

For research use only. We do not sell to patients.

DNA, d(G-sp-G-sp-G-G-G-A-C-G-A-T-C-G-T-C-G-sp-G-sp-G-sp-G-sp-G-sp-G), sodium salt

ODN 2216 sodium Chemical Structure

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Description

ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4+ T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4+ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8+ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus[1][2][3].

IC50 & Target

TLR9

 

In Vitro

ODN 2216 (sodium) (10 μM; 16 h pre-treatment, 9 days co-culture, 48 h cytotoxicity assay) does not significantly enhance MamA2.1-specific activation of primary HLA-A2+ CD8+ T cells or subsequent MamA-specific cytotoxicity against AU565 breast cancer cells compared to MamA2.1 peptide alone[1].
ODN 2216 (sodium) (3 μM; 24 h) induces TLR9-mediated IFN-α secretion by human PBMCs after 24 hours of incubation at a concentration of 3 μM[2].
ODN 2216 (sodium) (0.5-10 μM; 4 days) dose-dependently increases intracellular ATP and IL-6 levels in human PBMCs[2].
ODN 2216 (sodium) (500 ng/mL; 14 hours) physically interacts with intracellular TLR9 in lysosomes of human CD4+ CD25- T cells following 14-hour incubation with 500 ng/mL ODN 2216 FITC[3].
ODN 2216 (sodium) (500 ng/mL; 72 hours) induced increased proliferation of human CD4+ CD25- T cells, which is dependent on TLR9 signaling via TLR9, MyD88, IRAK1, and TRAF3, but not IRF7[3].
ODN 2216 (sodium) (500 ng/mL; 48 hours) treated human CD4+ CD25- T cells acquire dose-dependent suppressive activity against untreated autologous CD4+ T cells, with maximum suppression (48.57%) at a 4:1 suppressor:responder ratio[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: MamA2.1-specific activation of primary HLA-A2+ CD8+ T cells or subsequent MamA-specific cytotoxicity against AU565 breast cancer cells
Concentration: 10 µM
Incubation Time: 16 h pre-treatment, 9 days co-culture, 48 h cytotoxicity assay
Result: Couldn't significantly enhance MamA2.1-specific activation of primary HLA-A2+ CD8+ T cells or subsequent MamA-specific cytotoxicity against AU565 breast cancer cells compared to MamA2.1 peptide alone.

ELISA Assay[2]

Cell Line: human PBMC
Concentration: 0.5, 1, 5, 10 μM
Incubation Time: 4 days
Result: Dose-dependently increased intracellular ATP levels and IL-6 secretion in human PBMCs.
In Vivo

ODN 2216 (sodium) (100 μg/mouse; i.p.; 4 total doses at 2-week intervals) acts as an adjuvant to MamA2.1 peptide vaccination in HLA-A2/C57BL/6J mice, enhancing peritoneal macrophage IL-12p70, TLR9, and TLR6 expression, and increasing MamA2.1-specific CD8+ T cell activation, but does not significantly reduce AU565 breast tumor growth in SCID/beige mice following adoptive T cell transfer[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HLA-A2/C57BL/6J transgenic mice; SCID/beige mice (vaccinated with MamA2.1 peptide, adoptive CD8+ T cell transfer, orthotopically implanted 24-day old AU565 breast tumors)[1]
Dosage: 100 µg/mouse
Administration: i.p.; 4 total doses at 2-week intervals
Result: Demonstrated significantly enhanced IL-12p70 mRNA expression in peritoneal macrophages compared to MamA2.1 peptide alone groups.
Demonstrated significantly enhanced TLR9 mRNA expression in peritoneal macrophages compared to MamA2.1 peptide alone groups.
Demonstrated significantly enhanced TLR6 mRNA expression in peritoneal macrophages compared to MamA2.1 peptide alone groups.
Induced significantly enhanced MamA2.1 tetramer staining in CD8+ T cells compared to no peptide or MamA2.1 peptide alone groups.
Did not result in a significant reduction in tumor growth in SCID/beige mice following adoptive T cell transfer compared to MamA2.1 peptide alone groups.
Molecular Weight

6432 (free acid)

Appearance

Solid

Color

White to off-white

SMILES

[ODN 2216 (sodium)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 98.57%

References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
ODN 2216 sodium
Cat. No.:
HY-150741C
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