401479

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
• Empirical Formula (Hill Notation): C₉H₈N₂OS₂
• CAS Number: 354812-17-2
• Molecular Weight: 224.30
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3