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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||BMC Nephrol (2015). Figure 2. SC-514|
|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.|
A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts.
Kishore N, et al. J Biol Chem. 2003 Aug 29;278(35):32861-71. PMID: 12813046.
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LY2409881 is a novel selective inhibitor of IKK2 with IC50 of 30 nM; IC50 for IKK1 and other common kinases is at least one log higher.
PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
Bardoxolone is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.
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PHA-408 is a highly selective and ATP-competitive IKK-2 inhibitor with IC50 of 40 nM.
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