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SML2464

Sigma-Aldrich

KRN2

≥98% (HPLC)

Synonym(e):

KRN2, 13-[(2-Fluorophenyl)methyl]-5,6-dihydro-9,10-dimethoxy-benzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium chloride

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About This Item

Empirische Formel (Hill-System):
C27H23FClNO4
CAS-Nummer:
248260-75-5
Molekulargewicht:
479.93
MDL-Nummer:
MFCD31728343
UNSPSC-Code:
12352200

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated

Farbe

faint yellow to dark orange

Löslichkeit

H2O: 2 mg/mL, clear (warmed)

Lagertemp.

2-8°C

SMILES String

FC(C=CC=C1)=C1CC2=C([N+](CC3)=CC4=C2C=CC(OC)=C4OC)C5=C3C=C(OCO6)C6=C5.[Cl-]

Biochem./physiol. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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
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
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

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