For research use only. Not for therapeutic Use.
SC-514 (CAT: I003293), also known as GK 01140, is a selective inhibitor of IKK-2 (IκB kinase-2), a critical enzyme involved in the NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) signaling pathway. SC-514 specifically targets IKK-2 and does not inhibit other isoforms of IKK or other serine-threonine and tyrosine kinases. By selectively blocking the activity of IKK-2, SC-514 interferes with the activation of NF-κB, a transcription factor that plays a key role in regulating inflammation, immune responses, and cell survival.
| Catalog Number | I003293 |
| CAS Number | 354812-17-2 |
| Synonyms | 3-amino-5-thiophen-3-ylthiophene-2-carboxamide |
| Molecular Formula | C₉H₈N₂OS₂ |
| Purity | ≥95% |
| Target | IKK |
| Solubility | DMSO: ≥ 53 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 11.2±4.7uM [1] |
| InChI | InChI=1S/C9H8N2OS2/c10-6-3-7(5-1-2-13-4-5)14-8(6)9(11)12/h1-4H,10H2,(H2,11,12) |
| InChIKey | BMUACLADCKCNKZ-UHFFFAOYSA-N |
| SMILES | C1=CSC=C1C2=CC(=C(S2)C(=O)N)N |
| Reference | 1:Biochem Pharmacol. 2013 Dec 15;86(12):1775-83. doi: 10.1016/j.bcp.2013.09.017. Epub 2013 Sep 30. SC-514, a selective inhibitor of IKKβ attenuates RANKL-induced osteoclastogenesis and NF-κB activation.Liu Q,Wu H,Chim SM,Zhou L,Zhao J,Feng H,Wei Q,Wang Q,Zheng MH,Tan RX,Gu Q,Xu J,Pavlos N,Tickner J,Xu J, PMID: 24091016 DOI: 10.1016/j.bcp.2013.09.017 </br><span>Abstract:</span> The RANKL-induced NF-κB signaling pathway is essential for osteoclastogenesis. This study aims to identify specific inhibitors targeting NF-κB signaling pathway, which might serve as useful small molecule inhibitors for the treatment and alleviation of osteoclast-mediated bone lytic diseases. By screening for compounds that selectively inhibit RANKL-induced NF-κB activation in RAW264.7 cells as monitored by luciferase reporter gene assay, we identified SC-514, a specific inhibitor of IKKβ, as a candidate compound targeting osteoclastogenesis. SC-514 dose-dependently inhibits RANKL-induced osteoclastogenesis with an IC50 of <5μM. At high concentrations, SC-514 (≥12.5μM) induced apoptosis and caspase 3 activation in RAW264.7 cells. Moreover, SC-514 specifically suppressed NF-κB activity owing to delayed RANKL-induced degradation of IκBα and inhibition of p65 nuclear translocation. Taken together, our results indicate that SC-514 impairs RANKL-induced osteoclastogenesis and NF-κB activation. Thus, targeting IKKβ by SC-514 presents as a potential treatment for osteoclast-related disorders such as osteoporosis and cancer-induced bone loss. Copyright © 2013 Elsevier Inc. All rights reserved. |
