ACHP
Chemical Name: 2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile
Purity: ≥97%
Biological Activity
ACHP is a IκB kinase inhibitor (IC50 values are 8.5 and 250 nM for IKKβ and IKKα respectively). Selective for IKKα and IKKβ over IKK3, Syk and MAPKKK4 (IC50 values are > 20 μM). Inhibits DNA binding activity of NF-κB. Blocks NF-κB pathway in multiple myeloma cell lines; induces cell growth arrest and apoptosis. Also inhibits STAT3 signaling in NSCLC in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Induction of indoleamine 2, 3-dioxygenase in human dendritic cells by a cholera toxin B subunit-proinsulin vaccine.
Mbongue J, Nicholas D, Zhang K, Kim N, Hamilton B, Larios M, Zhang G, Umezawa K, Firek A, Langridge W
PLoS ONE, 2015;10(2):e0118562. -
NF-?B Signaling Pathway in Controlling Intervertebral Disk Cell Response to Inflammatory and Mechanical Stressors
Gwendolyn Sowa
Phys Ther, 2016;96(5):704-11. -
NKG2D receptor activation of NF-kappaB enhances inflammatory cytokine production in murine effector CD8(+) T cells.
Whitman E, Barber A
Mol Immunol, 2015;63(2):268-78. -
Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents.
Murata et al.
Bioorg.Med.Chem.Lett., 2004;14:4019 -
The IκB kinase inhibitor ACHP targets the STAT3 signaling pathway in human non-small cell lung carcinoma cells.
Lee et al.
Biomolecules, 2019;9:875 -
Growth inhibition of multiple myeloma cells by a novel IκB kinase inhibitor.
Sanda et al.
Clin.Cancer Res., 2005;11:1974
Product Datasheets
Citations for ACHP
The citations listed below are publications that use Tocris products. Selected citations for ACHP include:
12 Citations: Showing 1 - 10
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A naturally derived small molecule NDSM253 inhibits IKK1 to suppress inflammation response and promote bone healing after fracture.
Authors: Lin Et al.
Am J Transl Res 2021;13:24-37
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Histone H3.3 phosphorylation amplifies stimulation-induced transcription.
Authors: Miao Et al.
Nature 2020;583:852-857
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Patient-specific logic models of signaling pathways from screenings on cancer biopsies to prioritize personalized combination therapies.
Authors: Christoph A Et al.
Mol Syst Biol 2020;16:e8664
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The IκB kinase inhibitor ACHP targets the STAT3 signaling pathway in human non-small cell lung carcinoma cells.
Authors: Lee Et al.
Biomolecuces 2019;9:875
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Interleukin-1β Induces mtDNA Release to Activate Innate Immune Signaling via cGAS-STING.
Authors: Michael Et al.
Mol Cell 2019;74:801-815.e6
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Dysregulation of Gap Junction Function and Cytokine Production in Response to Non-Genotoxic Polycyclic Aromatic Hydrocarbons in an In Vitro Lung Cell Model.
Authors: Romo Et al.
Cancers (Basel) 2019;11
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An NFκB-dependent mechanism of tumor cell plasticity and lateral transmission of aggressive features.
Authors: Espinoza-Sánchez Et al.
Oncotarget 2018;9:26679
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A microfluidics platform for combinatorial drug screening on cancer biopsies.
Authors: Eduati Et al.
Nat Commun 2018;9:2434
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Cell line with endogenous EGFRvIII expression is a suitable model for research and drug development purposes.
Authors: Stec Et al.
Oncotarget 2016;7:31907
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Low CD38 Identifies Progenitor-like Inflammation-Associated Luminal Cells that Can Initiate Human Prostate Cancer and Predict Poor Outcome.
Authors: Liu Et al.
Cell Rep 2016;17:2596
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Induction of indoleamine 2, 3-dioxygenase in human dendritic cells by a cholera toxin B subunit-proIns vaccine.
Authors: Mbongue Et al.
Front Cell Neurosci 2015;10:e0118562
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The IκB kinase inhibitor ACHP strongly attenuates TGFβ1-induced myofibroblast formation and collagen synthesis.
Authors: Mia and Bank
J Cell Mol Med 2015;
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