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
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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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