| CAS NO: | 1186195-62-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1186195-62-9 |
| 别名 | IKK Inhibitor VII |
| 化学名 | [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone, monohydrochloride |
| Canonical SMILES | O=C(N1CCC(N2CCCC2)CC1)C3=CC=C(C=C3)NC4=NC=CC(C5=CC(C=CC=C6)=C6S5)=N4.Cl |
| 分子式 | C28H29N5OS o HCl |
| 分子量 | 520.1 |
| 溶解度 | ≤10mg/ml in DMSO;5mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 200, 40, and 70 nM for IKKα, IKKβ, and IKK complex, respectively. IKK-16 is an IκB kinases (IKKs) inhibitor. The IκB kinase (IKK), part of a high molecular weight protein complex consisting of three subunits, IKK1, IKK2, and IKKc, emerged as a prime target for the development of novel anti-rheumatic and anti-inflammatory drugs. In vitro: In screening study, it was found that compounds with an additional basic amino group were more active than the neutral inhibitors. The tertiary amines, such as IKK-16, was active in the low-nanomolar range. IKK-16 could inhibit TNFa-induced adhesion molecule expression in a potency range similar to the IjBa degradation. Although IKK-16 showed activity in the IFNc-induced expression of b2 microglobulin, its potency was weaker. These data demonstrated that IKK-16 had an effect on downstream gene expression, however, on the cellular level the selectivity was modest [1]. In vivo: Animal study found that the treatment with IKK 16 to mice could attenuate the impairment in systolic contractility, renal dysfunction, hepatocellular injury and lung inflammation in LPS/PepG-induced MOD and in polymicrobial sepsis. IKK-16 treatment could also significantly attenuated the increase in inducible nitric oxide synthase (iNOS) expression and increase the phosphorylation of Akt and endothelial nitric oxide synthase [2]. Clinical trial: So far, no clinical study has been conducted. References: |
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