| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
powder | [color ]
faint yellow to dark orange | [Water Solubility ]
H2O: 2mg/mL, clear (warmed) | [InChIKey]
RPHFGOXVJGNJJH-UHFFFAOYSA-M | [SMILES]
FC(C=CC=C1)=C1CC2=C([N+](CC3)=CC4=C2C=CC(OC)=C4OC)C5=C3C=C(OCO6)C6=C5.[Cl-] |
| Hazard Information | Back Directory | [Description]
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM. KRN2 shows much stronger inhibition of NFAT5-dependent reporter activity in RAW 264.7 macrophages than does BBR; the IC50 value is 0.1 μM for KRN2 and 4 μM for BBR. In parallel, 0.5 μM of KRN2 significantly suppresses the LPS-stimulated increase in NFAT5 protein expression in RAW 264.7 macrophages. It is confirmed that LPS-induced NFAT5 mRNA and protein expression is nearly completely blocked by KRN2. Similarly, KRN2 inhibits the translocation of NFAT5 into the nucleus of RAW264.7 cells stimulated with LPS. KRN2 specifically represses LPS-induced NFAT5 promoter activity, whereas it fails to reduce high salt-induced NFAT5 activity in the same cells, which is consistent with the selective inhibition of TLR4-activated NFAT5, but not hypertonicity-induced NFAT5, by KRN2[1]. | [Uses]
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis[1]. | [in vivo]
KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role[1].
KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration[1]. | Animal Model: | 8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freund's adjuvant[1]. | | Dosage: | 3 mg/kg. | | Administration: | Peritoneally (i.p.) daily for 2 weeks. | | Result: | Effective in suppressing AIA.
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| Animal Model: | 8-week-old DBA/1Jmice immunized with bovine type II collagen[1]. | | Dosage: | 3 mg/kg. | | Administration: | Peritoneally (i.p.) daily. | | Result: | Effective in suppressing CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.
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| [storage]
Store at -20°C | [References]
[1]. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273. |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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