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)
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
30.0mg/ml 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. IKK-16 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 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]

Protocol (from reference)

Customer Product Validation

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

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

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

Selleck's IKK-16 has been cited by 69 publications

FAT10 is phosphorylated by IKKβ to inhibit the antiviral type-I interferon response [ Life Sci Alliance, 2024, 10.26508/lsa.202101282] PubMed: 37940187
Serotonin reduction in post-acute sequelae of viral infection [ Cell, 2023, 186(22):4851-4867.e20] PubMed: 37848036
Intestinal epithelial HDAC3 and MHC class II coordinate microbiota-specific immunity [ J Clin Invest, 2023, 133(4)e162190] PubMed: 36602872
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding [ SCIENCE ADVANCES, 2023, Vol-9,-Issue-12] PubMed: None
Integrated single-cell (phospho-)protein and RNA detection uncovers phenotypic characteristics and active signal transduction of human antibody secreting cells [ Mol Cell Proteomics, 2023, S1535-9476(23)00001-4] PubMed: 36623694
Ectopic CH60 mediates HAPLN1-induced cell survival signaling in multiple myeloma [ Life Sci Alliance, 2023, 6(3)e202201636] PubMed: 36625202
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding [ Sci Adv, 2023, 9(12):eadd5028] PubMed: 36947620
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909] PubMed: none
The RNF26/CBX7 axis modulates the TNF pathway to promote cell proliferation and regulate sensitivity to TKIs in ccRCC [ Int J Biol Sci, 2022, 18(5):2132-2145] PubMed: 35342353
Proteomic identification of proliferation and progression markers in human polycythemia vera stem and progenitor cells [ Blood Adv, 2022, bloodadvances.2021005344] PubMed: 35008095

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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.

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