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Purity: ≥98%
INH14 is a novel, potent and cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. INH14 is a fragment-like compound that inhibits the toll-like receptor 2 (TLR2)-mediated inflammatory activity and other inflammatory pathways (i.e., TLR4, TNF-R and IL-1R). In this study, we determined the molecular target of INH14. Overexpression of proteins that are part of the TLR2 pathway in cells treated with INH14 indicated that the target lay downstream of the complex TAK1/TAB1. Immunoblot assays showed that INH14 decreased IkBα degradation in cells activated by lipopeptide (TLR2 ligand). These data indicated the kinases IKKα and/or IKKβ as the targets of INH14, which was confirmed with kinase assays (IC50 IKKα=8.97 μm; IC50 IKKβ=3.59 μm). Furthermore, in vivo experiments showed that INH14 decreased TNFα formed after lipopeptide-induced inflammation, and treatment of ovarian cancer cells with INH14 led to a reduction of NF-kB constitutive activity and a reduction in the wound-closing ability of these cells. These results demonstrate that INH14 decreases NF-kB activation through the inhibition of IKKs. Optimization of INH14 could lead to potent inhibitors of IKKs that might be used as antiinflammatory drugs.
| Targets |
NF-κB; TBK1 (IKKβ = 3.598 μM); IKKα (IC50 = 8.975 μM)
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| ln Vivo |
INH14 (5 µg/g, i.p. for 2 hours) decreases inflammation brought on by lipopeptide in mice[1].
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| Animal Protocol |
8-week old, male, pathogen-free C57BL/6J mice[1]
5 µg/g, one hour before Pam2CSK4 injection I.P. for 2 hours |
| References |
| Molecular Formula |
C15H16N2O
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|---|---|
| Molecular Weight |
240.3
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| Exact Mass |
240.13
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| Elemental Analysis |
C, 74.97; H, 6.71; N, 11.66; O, 6.66
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| CAS # |
200134-22-1
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| Related CAS # |
200134-22-1
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| PubChem CID |
295048
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
253
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CPCZNJSFVOOZOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H16N2O/c1-2-12-8-10-14(11-9-12)17-15(18)16-13-6-4-3-5-7-13/h3-11H,2H2,1H3,(H2,16,17,18)
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| Chemical Name |
1-(4-ethylphenyl)-3-phenylurea
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| Synonyms |
INH14; INH-14; INH 14
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~48 mg/mL (~199.9 mM)
Ethanol: ~18 mg/mL (~74.9 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1615 mL | 20.8073 mL | 41.6146 mL | |
| 5 mM | 0.8323 mL | 4.1615 mL | 8.3229 mL | |
| 10 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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