ACHPACHP
MedChemExpress (MCE)
HY-107592
406208-42-2
Please store the product under the recommended conditions in the Certificate of Analysis.
Room temperature in continental US
may vary elsewhere.
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies.
ACHP (0-100 µM
3 days) inhibits cell growth with mean IC50 of 26.8 µM in three myeloma cell lines (U266, NCUMM-2, ILKM-2)[1]. ACHP (10 µM
24 h) induces cycle arrest in U266 and NCUMM-2 cells[1]. ACHP (10, 50 µM
8 h) induces apoptosis in NCUMM-2 cells[1]. ACHP (0-50 µM
20 min) inhibits the phosphorylation of IkBa and p65 in MT-2 and ED-40515(-) cells[2].
ACHP (0.3, 1, 3 mg/kg
p.o.
single) exhibits anti-inflammatory activity in Arachidonic acid-induced ear edema mice model[3].
IKK-β 8.5 nM (IC50) IKK-α 250 nM (IC50)
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[1]. Sanda T, et al. Growth inhibition of multiple myeloma cells by a novel IkappaB kinase inhibitor. Clin Cancer Res. 2005 Mar 1
11(5):1974-82. [Content Brief]
[2]. Lee JH, et al. The IκB Kinase Inhibitor ACHP Targets the STAT3 Signaling Pathway in Human Non-Small Cell Lung Carcinoma Cells. Biomolecules. 2019 Dec 13
9(12):875. [Content Brief]
[3]. Murata T, et al. Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents. Bioorg Med Chem Lett. 2004 Aug 2
14(15):4019-22. [Content Brief]
[4]. Sanda T, et al. Induction of cell death in adult T-cell leukemia cells by a novel IkappaB kinase inhibitor. Leukemia. 2006 Apr
20(4):590-8. [Content Brief]