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SC-514 is a small molecule, orally active, ATP-competitive IKKβ inhibitor that displays > 10-fold selectivity over 28 other kinases, including JNK, p38, MK2 and ERK. SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer and IKK-2 homodimer similarly. SC-514 inhibits transcription of NF-kappa B-dependent genes in IL-1 beta-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner. SC-514 attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 (IC50s of 20, 20 and 8 μM, respectively) in synovial fibroblasts stimulated with interleukin (IL)-1β. SC-514 reduces iNOS induction and exhibits anti-inflammatory activity in vivo. SC-514 also reduces NF-κB-mediated expression of other genes, such as TLR2 in TNF-activated astrocytes.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
SC-514 purchased from AbMole
Molecular Weight | 224.3 |
Formula | C9H8N2OS2 |
CAS Number | 354812-17-2 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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