ACHP HCl

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Chemical Structure| 406209-26-5 同义名 : IKK-2 Inhibitor VIII;ACHP Hydrochloride
CAS号 : 406209-26-5
货号 : A543661
分子式 : C21H25ClN4O2
纯度 : 99%+
分子量 : 400.902
MDL号 : MFCD22124458
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(261.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ACHP Hydrochloride demonstrates strong inhibition of IKK-β (IC50: 8.5 nM) and shows cellular efficacy (IC50=40 nM in A549 cells). It inhibits IKK-α moderately with an IC50 of 250 nM and maintains high selectivity against other kinases, such as IKK3, Syk, and MKK4 (IC50>20,000 nM). Additionally, ACHP exhibits significant effectiveness in various cell-based assays. It blocks NF-κB-dependent reporter gene activity in TNFα-stimulated HEK293 cells and PMA/calcium ionophore-activated Jurkat T cells. However, ACHP does not inhibit PMA-induced AP-1 activation in MRC-5 cells or PMA/calcium ionophore-induced NF-κB-dependent reporter gene expression in Jurkat cells at doses above 10 μM. ACHP specifically disrupts NF-κB signaling by targeting IKK-β in live cells[1]. ACHP reduces cell proliferation in a dose-responsive manner. Cell lines active for Tax show greater sensitivity to ACHP compared to Tax-inactive cell lines and Jurkat cells (with IC50 values of 3.1±1.3 μM for Tax-active cell lines, 10.7±1.7 μM for Tax-inactive cell lines, and 23.6 μM for Jurkat, respectively), indicating a higher reliance on NF-κB for the growth of Tax-active cells than for Tax-inactive cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.47mL

2.49mL

1.25mL

24.94mL

4.99mL

2.49mL
参考文献

[1]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.

[2]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.