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| Replacement Information |
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| Empirical Formula | CAS # |
|---|---|
| C₁₂H₁₀FN₃O₂S | 507475-17-4 |
| Description | |
|---|---|
| Overview | A cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). A 10 mM (500 µg/179 µl) solution of IKK-2 Inhibitor IV (Cat. No. 401484) in DMSO is available. |
| Catalogue Number | 401481 |
| Brand Family | Calbiochem® |
| Synonyms | [5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1 |
| References | |
|---|---|
| References | Podolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373. Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17. Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4. |
| Product Information | |
|---|---|
| CAS number | 507475-17-4 |
| ATP Competitive | Y |
| Form | Pale yellow solid |
| Hill Formula | C₁₂H₁₀FN₃O₂S |
| Chemical formula | C₁₂H₁₀FN₃O₂S |
| Reversible | Y |
| Structure formula Image | |
| Applications |
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| Biological Information | |
|---|---|
| Primary Target | IKK-2 |
| Primary Target IC<sub>50</sub> | 18 nM against IKK-2 |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Safety Information according to GHS |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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