IKK-16

Catalog No.S2882 Batch:S288201

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Technical Data

Formula

C28H29N5OS
Molecular Weight 483.63 CAS No. 873225-46-8
Solubility (25°C)* In vitro DMSO 97 mg/mL (200.56 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 30.000mg/ml (62.03mM) Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description IKK-16 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. This compound also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM.
Targets
IKK2 [1]
(Cell-free assay)		 IKK complex [1]
(Cell-free assay)		 IKK1 [1]
(Cell-free assay)
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 this compound 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]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/16236504/

Customer Product Validation

Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.

Data from [ , , J Immunol, 2016, 197(3):726-35. ]

mBM-DCs were preincubated with the indicated inhibitors for 30 min and then treated with or without 20 mM dryocrassin. After 1 h of incubation, the cells were washed, followed by stimulation with 100 ng/ml LPS for 20 h. The detection of phosphorylated forms of IKK, JNK, and p38 MAPK by Western blot analysis with specific antibodies.

Data from [ , , Cell Transplant, 2014, 23(4-5): 641-56 ]

(B) Cells were treated with an IKK 16 (10 μmol/ml) for 1 hr. The cells were then cultured with TGF-β1 (20 ng/ml) and AT-RvD1 (20 ng/ml). After incubation, the gene expressions of Nrf2 and Smad7 were determined by RT-PCR. The effects of the Nrf2 and Smad7 gene expressions by AT-RvD1 in the TGF-β1-induced EndMT process had been altered.

Data from [ , , Biomol Ther (Seoul), 2016, 24(2):132-9. ]

Selleck's IKK-16 Has Been Cited by 83 Publications

Phosphorylation of H3.3 at Serine 31 acts as a switch of nucleosome dynamics for transcription [ Nucleic Acids Res, 2025, 53(17)gkaf891] PubMed: 40966506
Molecular control of PDPNhi macrophage subset induction by ADAP as a host defense in sepsis [ JCI Insight, 2025, e186456] PubMed: 39903516
TLR4 endocytosis and endosomal TLR4 signaling are distinct and independent outcomes of TLR4 activation [ EMBO Rep, 2025, 10.1038/s44319-025-00444-2] PubMed: 40204912
Nbeal2 Inactivation Triggers Abl1 Stabilisation and Dysregulated Subcellular Localisation of the Multi-Drug-Resistant Protein MDR1 (ABCB1) in Mast Cells [ Immunology, 2025, NONE] PubMed: 41111259
Monoclonal Antibodies to Thyrotropin Receptor With Thyroid-Stimulating Activity Activate the NF-κB Pathway to Induce Chemokine Expression [ J Cell Mol Med, 2025, 29(11):e70647] PubMed: 40500868
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis [ Sci Adv, 2025, 11(4):eadq2395] PubMed: 39841821
Genetic mechanisms of resistance to targeted KRAS inhibition [ bioRxiv, 2025, 2025.08.04.668444] PubMed: 40799582
Hypoxia-induced histone methylation and NF-κB activation in pancreas cancer fibroblasts promote EMT-supportive growth factor secretion [ bioRxiv, 2025, 2025.01.30.635486] PubMed: 39974981
Size- and polymer-dependent toxicity of amorphous environmentally relevant micro- and nanoplastics in human bronchial epithelial cells [ Microplast nanoplast, 2025, 5(1):19] PubMed: 40385552
Linear ubiquitination mediates coronavirus NSP14-induced NF-κB activation [ Cell Commun Signal, 2024, 22(1):573] PubMed: 39616385

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.