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经验公式(希尔记法):
C27H23FClNO4
化学文摘社编号:
分子量:
479.93
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
产品名称
KRN2, ≥98% (HPLC)
InChI key
RPHFGOXVJGNJJH-UHFFFAOYSA-M
SMILES string
FC(C=CC=C1)=C1CC2=C([N+](CC3)=CC4=C2C=CC(OC)=C4OC)C5=C3C=C(OCO6)C6=C5.[Cl-]
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
faint yellow to dark orange
solubility
H2O: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Biochem/physiol Actions
KRN2 is a specific and potent inhibitor of nuclear factor of activated T cells 5 (NFAT5) that inhibits formation of NF-κB p65-DNA complexes. KRN2 suppresses migration of Fibroblast-like synoviocytes stimulated with TGF-β. KRN2 ameliorates experimental arthritis in mice.
KRN2 or 13-(2-fluorobenzyl)-berberine is a berberine derivative that effectively blocks the invasiveness of fibroblast-like synoviocytes (FLS). It is stable and orally bioavailable. It suppresses the production of proinflammatory cytokines to ameliorate arthritis severity.
specific and potent inhibitor of nuclear factor of activated T cells 5 (NFAT5) that inhibits formation of NF-κB p65-DNA complexes
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Eun-Jin Han et al.
EBioMedicine, 18, 261-273 (2017-04-12)
Nuclear factor of activated T cells 5 (NFAT5) has been implicated in the pathogenesis of various human diseases, including cancer and arthritis. However, therapeutic agents inhibiting NFAT5 activity are currently unavailable. To discover NFAT5 inhibitors, a library of >40,000 chemicals
Naeun Lee et al.
Frontiers in immunology, 10, 270-270 (2019-03-16)
The nuclear factor of activated T cells (NFAT5), also known as a tonicity-responsive enhancer-binding protein, was originally identified as a key transcription factor involved in maintaining cellular homeostasis against hypertonic and hyperosmotic environments. Although NFAT5 has been expressed and studied
Inessa Yanovsky et al.
Journal of medicinal chemistry, 55(23), 10700-10715 (2012-11-16)
The cascade of events that occurs in Alzheimer's disease involving oxidative stress and the reduction in cholinergic transmission can be better addressed by multifunctional drugs than cholinesterase inhibitors alone. For this purpose, we prepared a large number of derivatives of
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