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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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Quality Control & MSDS

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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      

Protocol

Cell experiment [1]:

Cell lines

HUVEC cells

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

0.3-2μM

Applications

IKK-16 (IKK Inhibitor VII) inhibited IKK2 by the blockade of IκBα degradation and suppressed TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Moreover, IKK-16 also showed activity in the IFNγ-induced expression of the MHC molecules β2 microglobulin and HLA-DR, but its potency in these assays is 4- to 10-fold weaker than the adhesion molecules assay.

Animal experiment [1]:

Animal models

Rat model; thioglycollate-induced peritonitis model in the mouse

Dosage form

30 mg/kg, subcutaneous injection (sc) or oral administration for 5 h; or 10 mg/kg, sc

Applications

IKK-16 (IKK Inhibitor VII) inhibited TNFα release into plasma upon LPS-challenge in the rat model. Moreover, IKK-16 (IKK Inhibitor VII, 10 mg/kg, sc) resulted in a maximal inhibition of neutrophil extravasation in thioglycollate-induced peritonitis model.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

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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.