IKK-2 Inhibitor IV

Name: IKK-2 Inhibitor IV
Brand: MM
Price: 136 CHF

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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500 μG

CHF 136.00

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About This Item

Empirical Formula (Hill Notation):

C₁₂H₁₀FN₃O₂S

CAS Number:

507475-17-4

Molecular Weight:

279.29

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD09037541

Key Documents

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Product Name

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.

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

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

Quality Level

100

Related Categories

Bioactive Small Molecule Inhibitors

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1 of 4

This Item	401482	401484	401487
Sigma-Aldrich 401481 IKK-2 Inhibitor IV	Sigma-Aldrich 401482 IKK-2 Inhibitor V	Sigma-Aldrich 401484 IKK-2 Inhibitor IV	Sigma-Aldrich 401487 IKK-2 Inhibitor VIII
form solid	form solid	form liquid	form solid
assay ≥95% (HPLC)	assay ≥95% (HPLC)	assay ≥95% (HPLC)	assay ≥95% (HPLC)
manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. −20°C
storage condition OK to freeze, protect from light	storage condition OK to freeze, protect from light	storage condition OK to freeze, desiccated (hygroscopic), protect from light	storage condition OK to freeze, protect from light

Biochem/physiol Actions

Cell permeable: yes

Primary Target
IKK-2

Product competes with ATP.

Reversible: yes

Target IC₅₀: 18 nM against IKK-2

Disclaimer

Toxicity: Standard Handling (A)

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).

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.

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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