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Formula | C28H29N5OS |
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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) |
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* <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.) |
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. | ||||||
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Targets |
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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] |
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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] |
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.]
The PARP inhibitor rucaparib blocks SARS-CoV-2 virus binding to cells and the immune reaction in models of COVID-19 [ Br J Pharmacol, 2024, 10.1111/bph.17305] | PubMed: 39191429 |
FAT10 is phosphorylated by IKKβ to inhibit the antiviral type-I interferon response [ Life Sci Alliance, 2024, 10.26508/lsa.202101282] | PubMed: 37940187 |
Myeloperoxidase-deficient mice exposed to Zymosan exhibit severe neutrophilia and anemia with enhanced granulopoiesis and reduced erythropoiesis, accompanied by pulmonary inflammation [ Immunobiology, 2024, 229(5):152843] | PubMed: 39186867 |
Serotonin reduction in post-acute sequelae of viral infection [ Cell, 2023, 186(22):4851-4867.e20] | PubMed: 37848036 |
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 |
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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.