JNK-IN-7

Selective JNK inhibitor CAS# 1408064-71-0

JNK-IN-7

Catalog No. BCC1672----Order now to get a substantial discount!

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Quality Control of JNK-IN-7

Number of papers citing our products

Chemical structure

JNK-IN-7

3D structure

Chemical Properties of JNK-IN-7

Cas No. 1408064-71-0 SDF Download SDF
PubChem ID 57340685 Appearance Powder
Formula C28H27N7O2 M.Wt 493.56
Type of Compound N/A Storage Desiccate at -20°C
Synonyms JNK inhibitor
Solubility >24.7mg/mL in DMSO
Chemical Name 3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[4-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
SMILES CN(C)CC=CC(=O)NC1=CC=CC(=C1)C(=O)NC2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CN=CC=C4
Standard InChIKey RADRIIWGHYFWPP-WEVVVXLNSA-N
Standard InChI InChI=1S/C28H27N7O2/c1-35(2)17-5-9-26(36)31-24-8-3-6-20(18-24)27(37)32-22-10-12-23(13-11-22)33-28-30-16-14-25(34-28)21-7-4-15-29-19-21/h3-16,18-19H,17H2,1-2H3,(H,31,36)(H,32,37)(H,30,33,34)/b9-5+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of JNK-IN-7

DescriptionJNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.In Vitro:JNK-IN-7 is a relatively selective JNK inhibitor in cells. In addition to JNK 1, 2, 3, JNK-IN-7 also binds to IRAK1(IC50=14.1 nM), YSK4 (IC50=4.8 nM), ERK3 (IC50=22 nM), PIK3C3, PIP5K3 and PIP4K2C[1]. Expression of divalent metal-ion transporter 1 (DMT1) in HCT116 is demonstrated to be markedly decreased under stimulation with TNF for 24 and 48 h, while JNK-IN-7 can significantly reverse the decrease. TNF can down-regulate DMT1 expression, while JNK-IN-7 can markedly suppress this function[2].

References:
[1]. Zhang T, et al. Discovery of Potent and Selective Covalent Inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54. [2]. Wu W, et al. Divalent metal-ion transporter 1 is decreased in intestinal epithelial cells and contributes to the anemia in inflammatory bowel disease. Sci Rep. 2015 Nov 17;5:16344.

Protocol

Kinase experiment [1]:

Inhibitory activities

The cell-based kinase assays for c-Jun phosphorylation were carried out by using the LanthaScreen c-Jun (1-79) HeLa cell line stably express GFP-c-Jun 1-79 and GFP-ATF2 19-106, respectively. Phosphorylation was determined by measuring the TR-FRET between a terbium-labeled phospho-c-Jun specific antibody and GFP. The cells were plated in white tissue culture-treated 384-well plates at a density of 10,000 cells per well in 32 ml assay medium (Opti-MEM, supplemented with 0.5% charcoal/dextran-treated FBS, 100 U/ml penicillin, and 100 mg/ml streptomycin, 0.1 mM nonessential amino acids, 1 mM sodium pyruvate, 25 mM HEPES [pH 7.3], and lacking phenol red). After overnight incubation, cells were pretreated for 90 min with JNK-IN-7 (at indicated concentration) diluted in 4 ml assay buffer followed by 30 min of stimulation with 5 ng/ml of TNF-α in 4 ml assay buffer (final assay volume was 40 ml). The medium was then removed by aspiration, and the cells were lysed by adding 20 ml of lysis buffer (20 mM Tris-HCl [pH 7.6], 5 mM EDTA, 1% Nonidet P-40 substitute, 5 mM NaF, 150 mM NaCl, and 1:100 protease and phosphatase inhibitor mix, P8340 and P2850, respectively). The lysis buffer included 2 nM of the terbium-labeled anti-c-Jun (pSer73) detection antibodies. After allowing the assay to equilibrate for 60 min at room temperature, TR-FRET emission ratios were determined on a BMG Pherastar fluorescence plate reader using the following parameters: excitation at 340 nm, emission 520 and 490 nm; 100 ms lag time; 200 ms integration time; emission ratio = Em 520/Em 490. All data were analyzed and plotted using GraphPad Prism 4.

Cell experiment [2]:

Cell lines

Human IL-1R cells; RAW264.7 macrophages.

Preparation method

Dissolved and stored at -20℃ as 10 mM solutions in DMSO [2]. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1, 1, 10 mM; 1 h.

Applications

In human IL-1R cells, JNK-IN-7 inhibits IL-1β-stimulated phosphorylation of c-Jun and the activation of Pellino 1. In Pam3CSK4-stimulated RAW macrophages, JNK-IN-7 also inhibits the phosphorylation of c-Jun.

References:

[1]. Zhang T, Inesta-Vaquera F, Niepel M, et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol, 2012, 19(1): 140-154.

[2]. Goh ET, Arthur JS, Cheung PC, et al. Identification of the protein kinases that activate the E3 ubiquitin ligase Pellino 1 in the innate immune system. Biochem J, 2012, 441(1): 339-346.

JNK-IN-7 Dilution Calculator

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Preparing Stock Solutions of JNK-IN-7

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0261 mL 10.1305 mL 20.261 mL 40.5219 mL 50.6524 mL
5 mM 0.4052 mL 2.0261 mL 4.0522 mL 8.1044 mL 10.1305 mL
10 mM 0.2026 mL 1.013 mL 2.0261 mL 4.0522 mL 5.0652 mL
50 mM 0.0405 mL 0.2026 mL 0.4052 mL 0.8104 mL 1.013 mL
100 mM 0.0203 mL 0.1013 mL 0.2026 mL 0.4052 mL 0.5065 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on JNK-IN-7

JNK-IN-7 is a selective JNK inhibitor with IC50 values of 1.54 nM, 1.99 nM, 0.75 nM to JNK1, JNK2, JNK3, respectively. It also inhibits phosphorylation of c-Jun, which is a direct substrate of JNK kinase.

JNK-IN-8, an analog of JNK-IN-7 with an extra flag methyl, dramatically improved in selectivity and eliminated binding to IRAK1, PIK3C3, PIP4K2C and PIP5K3, comparing to JNK-IN-7. JNK-IN-7 and JNK-IN-8 require Cys116 for JNK2 inhibition. JNK-IN-7 can indeed inhibit IRAK-1 dependent E3 ligase activity of pellino, which plays an role in the Toll receptor signaling pathway in cells at relative high compound concentrations (1–10 mM).

The IRAK1 inhibitor JNK-IN-7 inhibited the IL-1-stimulated activation of Pellino 1 in IL-1R cells, but not the Pam3CSK4-stimulated activation of Pellino 1 in RAW264.7 macrophages. JNK-IN-7 also suppressed the phosphorylation of c-Jun in Pam3CSK4-stimulated RAW macrophages, but in contrast with IL-1R cells it did not affect the activation of Pellino 1.

References:
[1].  Zhang T, Inesta-Vaquera F, Niepel M et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54.
[2].  Goh ET, Arthur JS, Cheung PC et al. Identification of the protein kinases that activate the E3 ubiquitin ligase Pellino 1 in the innate immune system. Biochem J. 2012 Jan 1;441(1):339-46.

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References on JNK-IN-7

Divalent metal-ion transporter 1 is decreased in intestinal epithelial cells and contributes to the anemia in inflammatory bowel disease.[Pubmed:26572590]

Sci Rep. 2015 Nov 17;5:16344.

Divalent metal-ion transporter 1 (DMT1) has been found to play an important role in the iron metabolism and hemogenesis. However, little is known about the potential role of DMT1 in the pathogenesis of anemia from patients with inflammatory bowel disease (IBD). Herein, we investigated expression of DMT1 in the intestinal mucosa by quantitative real-time polymerase chain reaction (qRT-PCR) and immunohistochemistry, and found that DMT1 was significantly decreased in the inflamed mucosa of active IBD patients compared with that in those patients at remission stage and healthy controls. To further study the mechanism, we cultured HCT 116 cell line in vitro. Expression of DMT1 in HCT116 was demonstrated to be markedly decreased under stimulation with TNF for 24 and 48 h, while JNK inhibitor (JNK-IN-7) could significantly reverse the decrease. Interestingly, anti-TNF therapy successfully improved anemia in clinical responsive Crohn's disease patients, and DMT1 was found to be markedly up-regulated in intestinal mucosa. Taken together, our studies demonstrate that decreased expression of DMT1 in intestinal mucosa leads to compromised absorption and transportation of iron and that blockade of TNF could rescue anemia and promote DMT1 expression in gut mucosa. This work provides a therapeutic approach in the management of anemia in IBD.

Description

JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.

Keywords:

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