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Submit ReviewACHP 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.
分子量 | 364.44 |
公式 | C21H24N4O2 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.29 | 20 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 ACHP 的部分引用包括:
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
Mia and Bank (2015) The IκB kinase inhibitor ACHP strongly attenuates TGFβ1-induced myofibroblast formation and collagen synthesis. J Cell Mol Med PMID: 26337045
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
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
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
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
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
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
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