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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.
Patent. CN113512587B 2022 Mar 18.
Patent. CN113512587B
SC-514 purchased from AbMole
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
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Source | BMC Nephrol (2015). Figure 2. SC-514 |
| Method | Immunohistochemistry | |
| Cell Lines | mice | |
| Concentrations | 5 mg/kg body weight | |
| Incubation Time | 8 weeks | |
| Results | The renal cortex of SC-514-treated MRL/lpr mice also showed a similar extent of mesangial cell proliferation and fusion of podocytes, but no formation of partial cellular crescents and less electron-dense deposits in the mesangial region. |
| 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 |
| Related IκB/IKK Products |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
| Bay 11-7085
BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
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