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.
Sinônimo(s):
IKK-2 Inhibitor IV, [5-( p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
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About This Item
Fórmula empírica (Notação de Hill):
C12H10FN3O2S
Número CAS:
Peso molecular:
279.29
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
Produtos recomendados
Nível de qualidade
Ensaio
≥95% (HPLC)
forma
solid
fabricante/nome comercial
Calbiochem®
condição de armazenamento
OK to freeze
protect from light
cor
white to pale yellow
solubilidade
DMSO: 10 mg/mL
Condições de expedição
ambient
temperatura de armazenamento
2-8°C
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)
chave InChI
SAYGKHKXGCPTLX-UHFFFAOYSA-N
Descrição geral
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).
Ações bioquímicas/fisiológicas
Cell permeable: yes
Primary Target
IKK-2
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: 18 nM against IKK-2
Embalagem
Packaged under inert gas
Advertência
Toxicity: Standard Handling (A)
Reconstituição
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Outras notas
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.
Informações legais
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
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