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Sigma-Aldrich

IKK-2 Inhibitor, SC-514

The IKK-2 Inhibitor, SC-514, also referenced under CAS 354812-17-2, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

Synonym(s):

IKK-2 Inhibitor, SC-514, SC-514

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About This Item

Empirical Formula (Hill Notation):
C9H8N2OS2
CAS Number:
Molecular Weight:
224.30
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C9H8N2OS2/c10-6-3-7(5-1-2-13-4-5)14-8(6)9(11)12/h1-4H,10H2,(H2,11,12)

InChI key

BMUACLADCKCNKZ-UHFFFAOYSA-N

General description

A cell-permeable (thienothienyl)amino-acetamide compound that displays anti-inflammatory properties. Acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of IKK-2 (IC50 = ~ 3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2). Its specificity has been confirmed using a panel of 31 other kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 >200 µM). Shown to specifically block NF-κB-dependent gene expression, but not MAP kinase pathways, in stimulated synovial fibroblasts RASF. A 25 mM (1 mg/178 µl) solution of IKK-2 Inhibitor, SC-514 (Cat. No. 401485) in DMSO is also available.
A cell-permeable, potent, reversible, ATP-competitive and highly selective inhibitor of IKK-2 (IC50 ~3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2) that also displays anti-inflammatory properties. Specificity has been reported using a panel of 31 additional kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 >200 µM). Shown to specifically block NF-κB-dependent gene expression, but not MAP kinase pathways, in stimulated RASF synovial fibroblast cells. Does not inhibit the phosphorylation and activation of the IKK complex.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: 3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Baxter, A., et al. 2004 Bioorg. Med. Chem. Lett.14, 2817.
Kishore, N., et al. 2003. J. Biol. Chem.278, 32861.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3


Certificates of Analysis (COA)

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