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KRN5 is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 is a derivative of KRN2. KRN5 at a concentration of 1 μM inhibited the expressions of NFAT5, IL-6, MCP-1, and GM-CSF, which are NFAT5 target molecules , in RAW 264.7 macrophages stimulated with LPS.
KRN5 exhibits high oral bioavailability and metabolic stability, ameliorated experimentally induced arthritis in mice without serious adverse effects, decreasing pro-inflammatory cytokine production. Oral feeding of KRN5 every other day for 3 weeks from day 21 dose-dependently mitigated arthritis severity. When compared to methotrexate, a commonly used DMARD, the efficacy of oral KRN5 at 60 mg/kg was more potent in suppressing arthritis. The concentration of serum anti-type II collagen IgG also significantly decreased in the sera of KRN5-treated mice.
| Molecular Weight | 459.47 |
| Formula | C27H22FNO5 |
| CAS Number | 1800465-47-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NFAT Products |
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| NFAT Inhibitor-1 (VIVIT peptide)
NFAT Inhibitor-1 (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT), it is superior at inhibiting calcineurin-mediated dephosphorylation of NFAT1, NFAT2, and NFAT4 in cell extracts. |
| INCA-6
INCA-6 is a inhibitor of interaction between calcineurin and its substrate nuclear factor of activated T cells (NFAT). |
| (+)-Syringaresinol
(+)-Syringaresinol, a lignan, is a NFAT transcription factor inhibitor, with an IC50 of 329.4 μM. (+)-Syringaresinol also can be used for the research of lymphocytic leukemia. |
| Cyclosporin D
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc). |
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