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IKK-16 (IKK Inhibitor VII)Selective IκB kinase inhibitor

IKK-16 (IKK Inhibitor VII)

Catalog No. B1586
Size Price Stock Qty
10mg $120.00 In stock
50mg $470.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

IKK-16 (IKK Inhibitor VII)

Biological Activity

Description IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 values of 40 nM, 70 nM and 200 nM, respectively.
Targets IKK-2 IKK complex IKK-1      
IC50 40 nM 70 nM 200 nM      

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Chemical Properties

Cas No. 873225-46-8 SDF Download SDF
Chemical Name [4-[[4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
Canonical SMILES C1CCN(C1)C2CCN(CC2)C(=O)C3=CC=C(C=C3)NC4=NC=CC(=N4)C5=CC6=CC=CC=C6S5
Formula C28H29N5OS M.Wt 483.63
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IKK-16 (IKK Inhibitor VII) is a novel inhibitor of IκB kinase (IKK) with the IC50 values of 0.04μM, 0.2μM and 0.07μM for IKK2, IKK1 and IKK complex, respectively [1].

IKK-16 (IKK Inhibitor VII) is a 2-benzamido-pyrimidines and selective inhibitor of IκB kinase (IKK). IKK-16 has been reported to effectively inhibit TNFα release into plasma upon LPS-challenge in the rat. In addition, IKK-16 has been found to be active at thioglycollate-induced peritonitis model in the mouse. Furthermore, IKK-16 has revealed to be an orally bio-available in rats and mice, and have significant in vivo activity in an acute model of cytokine release [1].

References:
[1] Waelchli R1, Bollbuck B, Bruns C, Buhl T, Eder J, Feifel R, Hersperger R, Janser P, Revesz L, Zerwes HG, Schlapbach A.Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. Epub 2005 Oct 19.