401481
IKK-2 Inhibitor IV
The IKK-2 Inhibitor IV, also referenced under CAS 507475-17-4, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.
Synonym(s):
IKK-2 Inhibitor IV, [5-( p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
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About This Item
Empirical Formula (Hill Notation):
C12H10FN3O2S
CAS Number:
Molecular Weight:
279.29
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white to pale yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
Fc1ccc(cc1)c2[s]c(c(c2)C(=O)N)NC(=O)N
InChI
1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)
InChI key
SAYGKHKXGCPTLX-UHFFFAOYSA-N
General description
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.
A cell-permeable, reversible, ATP-competitive, and potent inhibitor of IKK-2 (IC50 = 18 nM) that exhibits 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). Shown to reduce paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IKK-2
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: 18 nM against IKK-2
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
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.
Karin, M., et al. 2004. Nat. Rev. Drug Discov.3, 17.
Roshak, A.K., et al. 2002. Inflamm. Res.51, S4.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
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