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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)
Citations (12)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

Do you know of a great paper that uses ACHP from Tocris? Please let us know.

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