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Merck
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401481

Sigma-Aldrich

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.

Szinonimák:

IKK-2 Inhibitor IV, [5-( p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez


About This Item

Tapasztalati képlet (Hill-képlet):
C12H10FN3O2S
CAS-szám:
Molekulatömeg:
279.29
MDL-szám:
UNSPSC kód:
12352200
NACRES:
NA.77

Minőségi szint

Teszt

≥95% (HPLC)

Forma

solid

gyártó/kereskedő neve

Calbiochem®

tárolási körülmény

OK to freeze
protect from light

szín

white to pale yellow

oldhatóság

DMSO: 10 mg/mL

kiszállítva

ambient

tárolási hőmérséklet

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)

Nemzetközi kémiai azonosító kulcs

SAYGKHKXGCPTLX-UHFFFAOYSA-N

Általános leírás

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).

Biokémiai/fiziológiai hatások

Cell permeable: yes
Primary Target
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: 18 nM against IKK-2

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Egyéb megjegyzések

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.

Jogi információk

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3


Analitikai tanúsítványok (COA)

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