| Bioactivity | 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[1][2][3][4]. |
| Invitro | ACHP (0-100 µM; 3 days) 抑制骨髓瘤细胞系 (U266, NCUMM-2, ILKM-2) 生长的平均 IC50 值为 26.8 µM[1]。ACHP (10 µM; 24 h) 诱导 U266 和 NCUMM-2 细胞周期停滞[1]。ACHP (10, 50 µM; 8 h) 诱导 NCUMM-2 细胞凋亡[1]。ACHP (0-50 µM; 20 min) 在 MT-2 and ED-40515(-) 细胞中抑制 IkBa 和 p65 的磷酸化[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ACHP 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | ACHP (0.3, 1, 3 mg/kg; p.o.; single) 在 Arachidonic acid 诱导的耳水肿小鼠模型中显示出抗炎活性[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 406208-42-2 |
| Formula | C21H24N4O2 |
| Molar Mass | 364.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [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. [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. |