Name | SC-514 |
Synonyms | SC-514 GK 01140 IKK-2 Inhibitor, SC-514 4-Amino-[2',3'-bithiophene]-5-carboxamide 5-(Thien-3-yl)-3-aminothiophene-2-carboxamide 3-amino-5-(thiophen-3-yl)thiophene-2-carboxamide |
CAS | 354812-17-2 |
Molecular Formula | C9H8N2OS2 |
Molar Mass | 224.3 |
Melting Point | 209-211°C |
Solubility | DMSO: soluble10mg/mL, clear |
Appearance | powder |
Color | white to light brown |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | SC-514 inhibited the activity of the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer and IKK-2 homodimer with similar strength. SC-514 inhibition of NF-κB-dependent IL-6,IL-8,COX-2 gene expression in il-1β-induced rheumatoid arthritis synovial fibroblasts (RASFs) with an IC50 of 20 μm, 20 M and 8 M. In RASFs, 100 μm SC-514 inhibits phosphorylation and degradation of IκBα and also reduces the amount of p65 translocated to the nucleus. |
In vivo study | In an acute model, SC-514 potently inhibited LPS-induced Serum TNF-alpha production. SC-514(50 mg/kg, I. P.) inhibited TNF-α production by up to 70%. |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.458 ml | 22.292 ml | 44.583 ml |
5 mM | 0.892 ml | 4.458 ml | 8.917 ml |
10 mM | 0.446 ml | 2.229 ml | 4.458 ml |
5 mM | 0.089 ml | 0.446 ml | 0.892 ml |
biological activity | SC-514 (GK 01140) is an orally potent, ATP-competitive IKK-2 inhibitor, the IC50 is 3-12 μm, which inhibits NF-κB dependent gene expression and does not inhibit other IKK isomers or other serine-threonine and tyrosine kinases. |
Target | Value |
IKK2 | 3 μM-12 μM |
CDK2/CyclinA | 61 μM |
AUR2 | 71 μM |
PRAK | 75 μM |
MSK () | 123 μM |
Use | A cell-permeable (thienothienyl)amino-acetamide. Acts as a pot, 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 things, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 > 200 μM). Shown to specifically block NF-kB-dependent gene expression, but not MAP kinase pathways, in stimulated synovial fibroblasts RASF. |