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IKK-16 (IKK Inhibitor VII)

Selective IκB kinase inhibitor CAS# 873225-46-8

IKK-16 (IKK Inhibitor VII)

Catalog No. BCC4555----Order now to get a substantial discount!

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Chemical structure

IKK-16 (IKK Inhibitor VII)

3D structure

Chemical Properties of IKK-16 (IKK Inhibitor VII)

Cas No. 873225-46-8 SDF Download SDF
PubChem ID 9549298 Appearance Powder
Formula C28H29N5OS M.Wt 483.63
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 27 mg/mL (55.83 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name [4-[[4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
SMILES C1CCN(C1)C2CCN(CC2)C(=O)C3=CC=C(C=C3)NC4=NC=CC(=N4)C5=CC6=CC=CC=C6S5
Standard InChIKey BWZJBXAPRCVCKQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H29N5OS/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31)
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of IKK-16 (IKK Inhibitor VII)

DescriptionIKK-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.
TargetsIKK-2IKK complexIKK-1   
IC5040 nM70 nM200 nM    

Protocol

Cell Assay [2]
SH-SY5Y cells are transduced with 25% (v/v) BacMam LRRK2-GFP G2019S and plated (20 µL/well, 20,000 cells/well) onto eight 384-well assay plates. Then 25% BacMam LRRK2-GFP G2019S transduced SH-SY5Y cells are incubated with indicated concentrations of indicated compounds (e.g., IKK 16, 0.01, 0.1, 1, 10 and 100 μM) for 90 min prior to the TR-FRET detection with Tb-anti-LRRK2 pSer935 antibody. The % inhibition is calculated[2].

Animal Administration [1][3]
Rats and Mice[1] IKK 16 is tested in two animal models. First, its efficacy to inhibit TNFα release into plasma upon LPS-challenge in the rat is determined. IKK 16 is dosed sc (30 mg/kg) or orally (30 mg/kg) 1 h prior to the LPS-challenge. Four hours after the challenge, plasma is collected and the systemic TNFα levels are analyzed using a commercially available ELISA kit. Both routes of administration of IKK 16 at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). In a second experiment, IKK 16 is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50% at a dose of 10 mg/kg sc. Mice[3] Two-month-old male C57BL/6 mice receive LPS (9 mg/kg body weight) and PepG (3 mg/kg body weight) in 0.9% saline (5 mL/kg body weight) intraperitoneally. Sham mice are not subjected to LPS/PepG, but are otherwise treated the same way. At 1 hour after LPS/PepG co-administration, mice are treated either with IKK 16 (1 mg/kg body weight i.v.) or vehicle (5 mL/kg body weight 10% DMSO i.v.). At 24 hours the experiment is terminated and organ and blood samples are collected for quantification of organ dysfunction and/or injury. Mice are randomly allocated into four different groups: (1) sham+vehicle (n=10); (2) sham+IKK 16 (n=3); (3) LPS/PepG+vehicle (n=9); (4) LPS/PepG+IKK 16 (n=10).

References:
[1]. Waelchli R, et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. [2]. Hermanson SB, et al. Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One. 2012;7(8):e43580. [3]. Coldewey SM, et al. Inhibition of IκB kinase reduces the multiple organ dysfunction caused by sepsis in the mouse. Dis Model Mech. 2013 Jul;6(4):1031-42.

IKK-16 (IKK Inhibitor VII) Dilution Calculator

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Preparing Stock Solutions of IKK-16 (IKK Inhibitor VII)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0677 mL 10.3385 mL 20.677 mL 41.3539 mL 51.6924 mL
5 mM 0.4135 mL 2.0677 mL 4.1354 mL 8.2708 mL 10.3385 mL
10 mM 0.2068 mL 1.0338 mL 2.0677 mL 4.1354 mL 5.1692 mL
50 mM 0.0414 mL 0.2068 mL 0.4135 mL 0.8271 mL 1.0338 mL
100 mM 0.0207 mL 0.1034 mL 0.2068 mL 0.4135 mL 0.5169 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on IKK-16 (IKK Inhibitor VII)

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.

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Description

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

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