1. Immunology/Inflammation
  2. Nuclear Factor of activated T Cells (NFAT)
  3. KRN2

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.

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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Based on 1 publication(s) in Google Scholar

Other Forms of KRN2:

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1 Publications Citing Use of MCE KRN2

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  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

IC50: 100 nM (NFAT5)[1].

In Vitro

KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions[1].
KRN2 dose-dependently inhibits the NF-κB p65 binding to Nfat5 promoter 1 and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1[1].

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

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].

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

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.
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.
Molecular Weight

479.93

Formula

C27H23ClFNO4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0836 mL 10.4182 mL 20.8364 mL 52.0909 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL 10.4182 mL
10 mM 0.2084 mL 1.0418 mL 2.0836 mL 5.2091 mL
15 mM 0.1389 mL 0.6945 mL 1.3891 mL 3.4727 mL
20 mM 0.1042 mL 0.5209 mL 1.0418 mL 2.6045 mL
25 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0836 mL
30 mM 0.0695 mL 0.3473 mL 0.6945 mL 1.7364 mL
40 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
50 mM 0.0417 mL 0.2084 mL 0.4167 mL 1.0418 mL
60 mM 0.0347 mL 0.1736 mL 0.3473 mL 0.8682 mL
80 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6511 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5209 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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KRN2
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HY-112125
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