| Identification | Back Directory | [Name]
N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamidehydrochloride | [CAS]
1186195-62-9 | [Synonyms]
IKK 16
CS-933
IKK-16 HCl
IKK16/IKK-16
IKK 16, >=98%
IKK-16 (hydrochloride)
N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamidehydrochloride
[4-[(4-Benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone hydrochloride (1:1) | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C28H31ClN6OS | [MDL Number]
MFCD09971091 | [MOL File]
1186195-62-9.mol | [Molecular Weight]
535.103 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
≤10mg/ml in DMSO;5mg/ml in dimethyl formamide | [form ]
crystalline solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
IKK-16 Hydrochloride is a potential novel IκB kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders. | [Biological Activity]
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]. | [IC 50]
200, 40, and 70 nm for ikkα, ikkβ, and ikk complex, respectively. | [storage]
Store at -20°C | [References]
[1] waelchli, r. ,bollbuck, b.,bruns, c., et al. design and preparation of 2-benzamido-pyrimidines as inhibitors of ikk. bioorganic & medicinal chemistry letters 16(1), 108-112 (2006).
[2] coldewey, s. m.,rogazzo, m.,collino, m., et al. inhibition of i k b kinase reduces the multiple organ dysfunction caused by sepsis in the mouse. dis.model mech. 6, 1031-1042 (2013). |
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