IKK-16 (hydrochloride)
Catalogue Number: C4569-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C28H29N5OS HCl |
| Physical state: | A crystalline solid |
| Type: | Kinase Inhibitors |
| Alias: | IKK Inhibitor VII |
| Shipping Condition: | Blue Ice |
| Unit(s): | 10 mg, 25 mg, 5 mg, 50 mg |
Description
Description: 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:[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).
Additional Text
Storage Note
Store at -20°C
Solubility
≤10mg/ml in DMSO;5mg/ml in dimethyl formamide
Smile String
O=C(N1CCC(N2CCCC2)CC1)C3=CC=C(C=C3)NC4=NC=CC(C5=CC(C=CC=C6)=C6S5)=N4.Cl
C4569 CofA
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