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SC-514

Cat. No. M2060
SC-514 Structure
Synonym:

GK 01140

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 60 In stock
50mg USD 220 In stock
100mg USD 340 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 224.3
Formula C9H8N2OS2
CAS Number 354812-17-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SC-514, GK 01140 supplier, IκB/IKK, inhibitors

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