IKKα inhibitors(component of inhibitor of nuclear factor kappa B kinase complex inhibitors), IKKβ inhibitors(inhibitor of nuclear factor kappa B kinase subunit beta inhibitors)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Inflammation

Originator Organization

Medical University of Innsbruck

Active Organization-

Inactive Organization

Medical University of Innsbruck

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC15H16N2O

InChIKeyCPCZNJSFVOOZOG-UHFFFAOYSA-N

CAS Registry200134-22-1

100 Clinical Results associated with INH14

100 Translational Medicine associated with INH14

100 Patents (Medical) associated with INH14

Literatures (Medical) associated with INH14

01 Mar 2025·Journal of Ethnopharmacology

Mechanism of Qingjie Fuzheng Granules in inhibiting colitis associated colorectal cancer by regulating TLR4 and IL-4R mediated macrophage polarization

Article

Author: Lin, Jiumao ; Chen, Xuzheng ; He, Jiajun ; Liu, Haiqin ; Wang, Shunyong ; Zhang, Youquan ; Zhong, Hangyan ; Guo, Kangyue ; Huang, Yunmei ; Jiang, Zhishan ; Lin, Ying ; Yang, Ruiming

ETHNOPHARMACOLOGICAL RELEVANCEQingjie Fuzheng Granules (QFG), a herbal formula, has been employed as an adjuvant therapy for colitis-associated colorectal cancer (CAC), yet the underlying mechanisms by which QFG operates remain unclear.AIMS OF THE STUDYThe aim of this study is to investigate whether the potential mechanism of QFG against CAC is associated with macrophage polarization.MATERIALS AND METHODSNon-targeted metabolomics and molecular docking assessed potential compounds of QFG to interact with targets associated with macrophage polarization. A model of AOM/DSS-induced CAC mice was established to analyze the effects of QFG on macrophage polarization using flow cytometry and immunohistochemical staining. In vitro experiments involved models of Ana-1 macrophages, either induced by varying QFG concentrations or with MD2 knockdown, to analyze M1-like phenotype. Meanwhile, M2-like macrophages models induced by IL-4 or culture supernatant of CT26 cells were utilized to assess the effects of QFG on M2-like macrophages. Finally, the mRNA expression of M1-like phenotype related to TLR4 pathways and the protein expression in IL-4R-mediated pathways were analyzed using RT-qPCR and Western blot, respectively.RESULTSMolecular docking confirmed the presence of binding sites between the ingredients of QFG and IL-4R or TLR4/MD2 receptor complex. QFG could induce a shift in macrophages towards an M1-like phenotype while inhibiting an M2-like phenotype in the colon with CAC mice and Ana-1 macrophages. QFG resulted in the upregulation of iNOS, IL-6, IL-1β, and TNF-α mRNA expression, which could be counteracted by TAK242, SR11302, INH14, PDTC, and LY294002, or by the knockdown of MD2. Meanwhile, QFG inhibited IL-4R-induced phosphorylation of STAT 6 and Akt.CONCLUSIONVarious monomer components within QFG can bind to MD2 or IL-4R, respectively, thereby inducing macrophages towards an M1-like phenotype through TLR4-mediated NF-κB, MAPK, and PI3K/Akt pathway activation, or inhibiting macrophages towards an M2-like phenotype via IL-4R-mediated JAKs pathway inhibition, ultimately exerting an inhibitory effect on the occurrence and development of CAC.

01 Mar 2019·ChemBioChemQ4 · BIOLOGY

INH14, a Small‐Molecule Urea Derivative, Inhibits the IKKα/β‐Dependent TLR Inflammatory Response

Q4 · BIOLOGY

Article

Author: Drexel, Meinrad ; Santos‐Sierra, Sandra ; Kirchmair, Johannes

AbstractN‐(4‐Ethylphenyl)‐N′‐phenylurea (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.

01 Jun 2016·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Synthesis of N -1′, N -3′-disubstituted spirohydantoins and their anticonvulsant activities in pilocarpine model of temporal lobe epilepsy

Q4 · MEDICINE

Article

Author: Yang, Chen ; Yoganathan, Sabesan ; Stephani, Ralph A ; Schanne, Francis A X

Herein we report the synthesis and anticonvulsant activity of a library of eighteen new compounds that are structural mimics of phenytoin. These class of compounds contain a N-1', N-3'-disubstituted spirohydantoin scaffold, where the N-1' and N-3' positions are modified with an alkyl group or aryl group. Of the eighteen compounds synthesized and tested, compound 5c showed the best anticonvulsant activity. It completely prevented the precursor events of motor seizure in the pilocarpine model of temporal lobe epilepsy. Additionally, ten of the analogs were more effective than phenytoin when compared using the Racine's score in the pilocarpine model. Based on the structure activity relationship (SAR), we concluded that alkyl groups (ethyl, propyl or cyclopropyl) at N-3' position and 4-nitro phenyl group at N-1' position are desirable.

100 Deals associated with INH14

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Preclinical	Austria	Medical University of Innsbruck	29 Jan 2019

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

INH14

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation