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この商品について
実験式(ヒル表記法):
C9H8N2OS2
CAS番号:
分子量:
224.30
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
SMILES string
[s]1c(cc(c1C(=O)N)N)c2c[s]cc2
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
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
Preparation Note
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.
Kishore, N., et al. 2003. J. Biol. Chem.278, 32861.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
保管分類
11 - Combustible Solids
一体何が起きているの?
WGK 3
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
401479-VMG: + 401479-1MG: + 401479-50MG:
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