| ACHPIκB kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | U266 and NCUMM-2 myeloma cell lines |
Preparation method | The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-50 μM; 8 h |
Applications | In U266 and NCUMM-2 myeloma cell lines, ACHP (>10 μmol/L) inhibited the DNA binding activity of NF-κB after only 4 hours. ACHP also efficiently inhibited the phosphorylation of IκBαand p65 at 1 μmol/L after 20 minutes treatment. ACHP (10 μmol/L, 24h) also inhibited cell cycle progression and induced apoptosis. In NCUMM-2 cells, ACHP (10 μmol/L) efficiently induced apoptosis (15.8%) and a higher concentration of ACHP (50 μmol/L) induced apoptosis in 43.7% of the cells. |
References: [1] Sanda T, Iida S, Ogura H, Asamitsu K, Murata T, Bacon KB, Ueda R, Okamoto T. Growth inhibition of multiple myeloma cells by a novel IkappaB kinase inhibitor. Clin Cancer Res. 2005 Mar 1;11(5):1974-82. | |
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| Cas No. | 406208-42-2 | SDF | Download SDF |
| Chemical Name | (E)-2-amino-6-(2-(cyclopropylmethoxy)-6-oxocyclohexa-2,4-dien-1-ylidene)-4-(piperidin-4-yl)-1,6-dihydropyridine-3-carbonitrile | ||
| Canonical SMILES | O=C1/C(C(OCC2CC2)=CC=C1)=C3NC(N)=C(C#N)C(C4CCNCC4)=C/3 | ||
| Formula | C21H24N4O2 | M.Wt | 364.44 |
| Solubility | <7.29mg l="" in="" dmso=""> | Storage | Store at -20°C |
| Physical Appearance | Yellow solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 8.5 and 250 nM for IKKβ and IKKα, respectively
ACHP is an IκB kinase inhibitor. Nuclear factor-KB (NF-KB) involved in cell survival and proliferation of multiple myeloma has been well established.
In vitro: ACHP is selective for IKKα and IKKβ over IKK3, Syk and MAPKKK4 (IC50 > 20 μM), DNA binding activity of NF-κB is inhibited. ACHP is an effective blockade NF-κB pathway in multiple myeloma cell lines, and induces cell growth arrest and apoptosis. It was observed that NF-KB is constitutively activated in all human myeloma cell lines, thus confirming the previous studies. In addition, It was found the phosphorylation of p65 subunit of NF-KB besides the phosphorylation of IKBA and the activation of NF-KB DNA binding and that various target genes of NF-KB including bcl-xL, XIAP, c-IAP1, cyclin D1, and IL-6 are up-regulated. 2-amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-piperidin-4-yl nicotinenitrile (ACHP) is a novel IKB kinase inhibitor. Treatment of myeloma cells with ACHP showed the cell growth was efficiently inhibited (IC50 values ranging from 18 to 35 Mmol/L) concomitantly with inhibition of the phosphorylation of IKBA/p65 and NF-KB DNA-binding, down-regulation of the NF-KB target genes, and then induction of apoptosis. In addition, the treatment of ACHP potentiated the cytotoxic effects of vincristine and melphalan (L-phenylalanine mustard), conventional antimyeloma drugs. These findings suggest that by blocking the antiapoptotic nature of myeloma cells endowed by the constitutive activation of NF-KB, IKB kinase inhibitors such as ACHP can sensitize myeloma cells to the cytotoxic effects of chemotherapeutic agents.
In vivo: So far, no study in vivo has been conducted.
Clinical trial: Clinical study has been conducted.
Reference:[1] Sanda T, Iida S, Ogura H, Asamitsu K, Murata T, Bacon KB, Ueda R, Okamoto T. Growth inhibition of multiple myeloma cells by a novel IkappaB kinase inhibitor. Clin Cancer Res. 2005 Mar 1;11(5):1974-82.
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上海好多的供应商的，具体还是看你选择了，其实试剂盒产品都差不多，什么远慕生物，古朵生物...好多的额
用双氧水去除过氧化物酶时，我是自己配的3%双氧水滴到片上而非将片浸入双氧水，这样可否？
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现在打算换中衫的试剂盒，代理商说中衫的试剂盒包括了二抗和DAB，想请教一下该试剂盒的具体内容有些什么？
万分感谢！
