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Description: Selective IKKα and IKKβ inhibitor
Chemical Name: 2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile
Purity: ≥97% (HPLC)
Biological Activity for ACHP
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 for ACHP
| M. Wt | 364.44 |
| Formula | C21H24N4O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 406208-42-2 |
| PubChem ID | 65663 |
| InChI Key | SRVFFFJZQVENJC-IHRRRGAJSA-N |
| Smiles | OC1=CC=CC(OCC3CC3)=C1C2=NC(N)=C(C#N)C(C4CCNCC4)=C2 |
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.
Solubility Data for ACHP
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.29 | 20 |
Preparing Stock Solutions for ACHP
The following data is based on the product molecular weight 364.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.72 mL | 68.6 mL | 137.2 mL |
| 1 mM | 2.74 mL | 13.72 mL | 27.44 mL |
| 2 mM | 1.37 mL | 6.86 mL | 13.72 mL |
| 10 mM | 0.27 mL | 1.37 mL | 2.74 mL |
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Product Datasheets for ACHP
References for ACHP
References are publications that support the biological activity of the product.
Sanda et al (2005) Growth inhibition of multiple myeloma cells by a novel IκB kinase inhibitor. Clin.Cancer Res. 11 1974 PMID: 15756023
Murata et al (2004) Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents. Bioorg.Med.Chem.Lett. 14 4019 PMID: 15225718
Lee et al (2019) The IκB kinase inhibitor ACHP targets the STAT3 signaling pathway in human non-small cell lung carcinoma cells. Biomolecules 9 875 PMID: 31847229
If you know of a relevant reference for ACHP, please let us know.
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Keywords: ACHP, ACHP supplier, IkappaB, IKB, kinase, IKKalpha, IKKa, IKKbeta, IKKb, inhibitors, inhibits, NF-kB, pathway, apoptosis, inducers, cell, growth, arrest, anticancer, IkB, Kinase, NF-kB/IkB, 4547, Tocris Bioscience
12 Citations for ACHP
Citations are publications that use Tocris products. Selected citations for ACHP include:
Lee et al (2019) The IκB kinase inhibitor ACHP targets the STAT3 signaling pathway in human non-small cell lung carcinoma cells. Biomolecuces 9 875 PMID: 31847229
Michael et al (2019) Interleukin-1β Induces mtDNA Release to Activate Innate Immune Signaling via cGAS-STING. Mol Cell 74 801-815.e6 PMID: 30952515
Liu et al (2016) Low CD38 Identifies Progenitor-like Inflammation-Associated Luminal Cells that Can Initiate Human Prostate Cancer and Predict Poor Outcome. Cell Rep 17 2596 PMID: 27926864
Christoph A et al (2020) Patient-specific logic models of signaling pathways from screenings on cancer biopsies to prioritize personalized combination therapies. Mol Syst Biol 16 e8664 PMID: 32073727
Miao et al (2020) Histone H3.3 phosphorylation amplifies stimulation-induced transcription. Nature 583 852-857 PMID: 32699416
Espinoza-Sánchez et al (2018) An NFκB-dependent mechanism of tumor cell plasticity and lateral transmission of aggressive features. Oncotarget 9 26679 PMID: 29928478
Eduati et al (2018) A microfluidics platform for combinatorial drug screening on cancer biopsies. Nat Commun 9 2434 PMID: 29934552
Mbongue et al (2015) Induction of indoleamine 2, 3-dioxygenase in human dendritic cells by a cholera toxin B subunit-proIns vaccine. Front Cell Neurosci 10 e0118562 PMID: 25714914
Lin et al (2021) A naturally derived small molecule NDSM253 inhibits IKK1 to suppress inflammation response and promote bone healing after fracture. Am J Transl Res 13 24-37 PMID: 33527006
Mia and Bank (2015) The IκB kinase inhibitor ACHP strongly attenuates TGFβ1-induced myofibroblast formation and collagen synthesis. J Cell Mol Med PMID: 26337045
Romo et al (2019) Dysregulation of Gap Junction Function and Cytokine Production in Response to Non-Genotoxic Polycyclic Aromatic Hydrocarbons in an In Vitro Lung Cell Model. Cancers (Basel) 11 PMID: 31018556
Stec et al (2016) Cell line with endogenous EGFRvIII expression is a suitable model for research and drug development purposes. Oncotarget 7 31907 PMID: 27004406
Do you know of a great paper that uses ACHP from Tocris? Please let us know.
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