IKK-16 (IKK Inhibitor VII)

Catalog No.S2882

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

Price Stock Quantity  
USD 220 In stock
USD 170 In stock
USD 670 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

IKK-16 (IKK Inhibitor VII) Chemical Structure

IKK-16 (IKK Inhibitor VII) Chemical Structure
Molecular Weight: 483.63

Validation & Quality Control

Customer Product Validation(1)

Quality Control & MSDS

Related Compound Libraries

IKK-16 (IKK Inhibitor VII) is available in the following compound libraries:

IκB/IKK Inhibitors with Unique Features

  • Selective IKK Inhibitor

    BAY 11-7082 IKK-1-selective, IC50=10 μM.

  • Most Potent IKK Inhibitor

    TPCA-1 IKK-2, IC50=17.9 nM.

  • IKK Inhibitor in Clinical Trial

    Bardoxolone Methyl Phase III for Chronic Kidney Disease and Type 2 Diabetes.

  • Newest IKK Inhibitor

    Bay 11-7085 Irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

Product Information

  • Compare IκB/IKK Inhibitors
    Compare IκB/IKK Products
  • Research Area
  • Inhibition Profile

Product Description

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 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively.
Targets IKK2 [1]
(Cell-free assay)
IKK complex [1]
(Cell-free assay)
IKK1 [1]
(Cell-free assay)
IC50 40 nM 70 nM 200 nM
In vitro IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker. [1]
In vivo IKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.[1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Waelchli R, et al. Bioorg Med Chem Lett, 2006, 16(1), 108-112.

Chemical Information

Download IKK-16 (IKK Inhibitor VII) SDF
Molecular Weight (MW) 483.63
Formula

C28H29N5OS

CAS No. 873225-46-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 97 mg/mL (200.56 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Methanone, [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-

Customer Product Validation (1)


Click to enlarge
Rating
Source Cell Transplant, 2014, 23(4-5): 641-56. IKK-16 (IKK Inhibitor VII) purchased from Selleck
Method Western Blot
Cell Lines mBM-DCs
Concentrations 5 mM
Incubation Time 30 min
Results Blocking the activities of IKK, JNK, and p38 MAPK with the inhibitors IKK-16, SP600125, and SB202190, respectively, completely abrogated the capacity of dryocrassin to retard DC-induced allogeneic T-cell proliferation.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related IκB/IKK Products

  • WS3

    WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

  • LY2409881

    LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.

  • AZD3264

    AZD3264 is a novel IKK2 inhibitor.

  • BAY 11-7082

    BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. Also inhibiting components of the ubiquitin system.

  • BMS-345541

    BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively.

  • Bardoxolone Methyl

    Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.

    Features:The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.

  • IMD 0354

    IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

  • TPCA-1

    TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1.

  • Bay 11-7085

    BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

  • SC-514

    SC-514 is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

Recently Viewed Items

Tags: buy IKK-16 (IKK Inhibitor VII) | IKK-16 (IKK Inhibitor VII) supplier | purchase IKK-16 (IKK Inhibitor VII) | IKK-16 (IKK Inhibitor VII) cost | IKK-16 (IKK Inhibitor VII) manufacturer | order IKK-16 (IKK Inhibitor VII) | IKK-16 (IKK Inhibitor VII) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us