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Cot inhibitor-1

COT/Tpl2 inhibitor CAS# 915365-57-0

Cot inhibitor-1

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Catalog No. BCC1496----Order now to get a substantial discount!

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Cot inhibitor-1

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Chemical Properties of Cot inhibitor-1

Cas No. 915365-57-0 SDF Download SDF
PubChem ID 11584834 Appearance Powder
Formula C27H27Cl2FN8 M.Wt 553.47
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 25 mg/mL (45.17 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 6-[[1-[2-(azepan-1-yl)ethyl]triazol-4-yl]methylamino]-8-chloro-4-(3-chloro-4-fluoroanilino)quinoline-3-carbonitrile
SMILES C1CCCN(CC1)CCN2C=C(N=N2)CNC3=CC(=C4C(=C3)C(=C(C=N4)C#N)NC5=CC(=C(C=C5)F)Cl)Cl
Standard InChIKey ZWFKJFUFYPOTKL-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H27Cl2FN8/c28-23-12-19(5-6-25(23)30)34-26-18(14-31)15-33-27-22(26)11-20(13-24(27)29)32-16-21-17-38(36-35-21)10-9-37-7-3-1-2-4-8-37/h5-6,11-13,15,17,32H,1-4,7-10,16H2,(H,33,34)
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 Cot inhibitor-1

DescriptionCot inhibitor-1 is a COT/Tpl2 inhibitor.

References:
[1]. Wu, Junjun et al Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-production in human whole blood.Bioorganic & Medicinal Chemistry Letters (2009), 19(13), 3485-3488.

Cot inhibitor-1 Dilution Calculator

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Cot inhibitor-1 Molarity Calculator

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Preparing Stock Solutions of Cot inhibitor-1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8068 mL 9.0339 mL 18.0678 mL 36.1357 mL 45.1696 mL
5 mM 0.3614 mL 1.8068 mL 3.6136 mL 7.2271 mL 9.0339 mL
10 mM 0.1807 mL 0.9034 mL 1.8068 mL 3.6136 mL 4.517 mL
50 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.7227 mL 0.9034 mL
100 mM 0.0181 mL 0.0903 mL 0.1807 mL 0.3614 mL 0.4517 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 Cot inhibitor-1

Cot inhibitor-1 is a COT/Tpl2 inhibitor.

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References on Cot inhibitor-1

Identification of Targets of a New Nutritional Mixture for Osteoarthritis Management Composed by Curcuminoids Extract, Hydrolyzed Collagen and Green Tea Extract.[Pubmed:27275599]

PLoS One. 2016 Jun 8;11(6):e0156902.

OBJECTIVE: We have previously demonstrated that a mixture of curcuminoids extract, hydrolyzed collagen and green tea extract (COT) inhibited inflammatory and catabolic mediator's synthesis by osteoarthritic human chondrocytes. The objective of this study was to identify new targets of COT using genomic and proteomic approaches. DESIGN: Cartilage specimens were obtained from 12 patients with knee osteoarthritis. Primary human chondrocytes were cultured in monolayer until confluence and then incubated for 24 or 48 hours in the absence or in the presence of human interleukin(IL)-1beta (10-11M) and with or without COT, each compound at the concentration of 4 mug/ml. Microarray gene expression profiling between control, COT, IL-1beta and COT IL-1beta conditions was performed. Immunoassays were used to confirm the effect of COT at the protein level. RESULTS: More than 4000 genes were differentially expressed between conditions. The key regulated pathways were related to inflammation, cartilage metabolism and angiogenesis. The IL-1beta stimulated chemokine ligand 6, matrix metalloproteinase-13, bone morphogenetic protein-2 and stanniocalcin1 gene expressions and protein productions were down-regulated by COT. COT significantly decreased stanniocalcin1 production in basal condition. Serpin E1 gene expression and protein production were down-regulated by IL-1beta. COT reversed the inhibitory effect of IL-1beta. Serpin E1 gene expression was up-regulated by COT in control condition. CONCLUSION: The COT mixture has beneficial effect on osteoarthritis physiopathology by regulating the synthesis of key catabolic, inflammatory and angiogenesis factors. These findings give a scientific rationale for the use of these natural ingredients in the management of osteoarthritis.

Description

Cot inhibitor-1 is a COT/Tpl2 inhibitor.

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