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KRN2 

Cat. No.: HY-112125
Handling Instructions

KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.

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

KRN2 Chemical Structure

KRN2 Chemical Structure

CAS No. : 248260-75-5

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  • Biological Activity

  • Protocol

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  • References

Description

KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.

IC50 & Target

IC50: 0.1 μM (NFAT5)[1].

In Vitro

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0836 mL 10.4182 mL 20.8364 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL
10 mM 0.2084 mL 1.0418 mL 2.0836 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

ROS production by RAW 264.7 cells stimulates with LPS (1 µg/mL) in the presence or absence of KRN2 (0.8 µM). ROS expression is determined by flow cytometry using a ROS probe. KRN2 (0.8 µM) is added to RAW 264.7 cells, which are then stimulated with LPS (1 µg/mL) in a time-dependent manner. Activity (%) of p38 isoform is measured in stable cell lines (CHO) in the presence of KRN2 or BBR, using a promoter reporter assay. Cells are treated with KRN2 in various doses (0.5, 1, 2, 5 μM) before stimulation with LPS (1 µg/mL) for 5 minutes and then fractionated into cytosolic extracts (upper panel) and nuclear extracts (lower panel)[1].

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

References
Molecular Weight

479.93

Formula

C₂₇H₂₃ClFNO₄

CAS No.

248260-75-5

SMILES

COC1=C(OC)C2=C[N+]3=C(C(C(CC3)=C4)=CC5=C4OCO5)C(CC6=CC=CC=C6F)=C2C=C1.[Cl-]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KRN2
Cat. No.:
HY-112125
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KRN2

Cat. No.: HY-112125