Selective, reversible and ATP-competitive inhibitor of IKK2 (IC50=11.2µM). Does not inhibit other IKK isoforms or other serine/threonine or tyrosine kinases. Inhibits transcription of NF-κB dependent genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent fashion.
Product Details
| Formula: | C9H8N2OS2 |
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| MW: | 224.3 |
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| CAS: | 354812-17-2 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | Yellow solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml) |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | If resuspended in solution, store at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Pharmacological inhibition of mTORC1 increases CCKBR-specific tumor uptake of radiolabeled minigastrin analogue [ 177 Lu]Lu-PP-F11N: M. Grzmil, et al.; Theranostics
10, 10861 (2020),
Abstract;
Full Text
Intermittent hypoxia-induced NF-κB and HO-1 regulation in human endothelial EA.hy926 cells: Q. Han, et al.; Cell Biochem. Biophys.
66, 431 (2013),
Application(s): Treatment of human endothelial EA.hy926 cell culture,
Abstract;
Involvement of metabotropic glutamate receptor 5, AKT/PI3K signaling and NF-kappaB pathway in methamphetamine-mediated increase in IL-6 and IL-8 expression in astrocytes: A. Shah, et al.; J. Neuroinflammation
9, 52 (2012),
Abstract;
A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts: N. Kishore, et al.; J. Biol. Chem.
278, 32861 (2003),
Abstract;
