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SC-514

In stock
Catalog No.
B1585
ATP-competitive IKK-2 inhibitor, orally active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$65.00
In stock
10mg
$50.00
In stock
50mg
$190.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

SC-514 is a cell-permeable and selective inhibitor of IKK-2 with IC50 value of 3-12μM [1, 2].

SC-514 inhibits all forms of recombinant human IKK-2 with IC50 values in the 3–12μM range. It also inhibits the native IKK complex. SC-514 specifically binds at the ATP-binding site of IKK-2 and exerts a reversible and competitive inhibition with ATP. However, SC-514 shows non-competitive inhibition with the IκB site. As an inhibitor of IKK-2, SC-514 is found to block the phosphorylation and degradation of IκBα and reduce the translocation level of p65 into the nucleus in IL-1β-treated RASFs. Additionally, SC-514 shows dose-dependent inhibition in the transcription of NF-κB-induced genes, including IL-6, IL-8, and COX-2. Moreover, SC-514 shows efficacious in reduction of LPS-induced TNFα production in the acute model of inflammation. SC-514 is also reported to inhibit the osteoclastogenesis in BMM cells through attenuating RANKL-induced activation of NF-κB [1, 2].

References:
[1] Kishore N, Sommers C, Mathialagan S, Guzova J, Yao M, Hauser S, Huynh K, Bonar S, Mielke C, Albee L, Weier R, Graneto M, Hanau C, Perry T, Tripp CS. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71.
[2] 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. SC-514, a selective inhibitor of IKKβ attenuates RANKL-induced osteoclastogenesis and NF-κB activation. Biochem Pharmacol. 2013 Dec 15;86(12):1775-83.

Chemical Properties

StorageStore at -20°C
M.Wt224.3
Cas No.354812-17-2
FormulaC9H8N2OS2
Solubility≥50.4mg/mL in DMSO
Chemical Name3-amino-5-thiophen-3-ylthiophene-2-carboxamide
SDFDownload SDF
Canonical SMILESC1=CSC=C1C2=CC(=C(S2)C(=O)N)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description SC-514 is an orally active, ATP-competitive inhibitor of IKK-2 with an IC50 value of 3-12 μM.
Targets IKK-2 CDK2/CyclinA AUR2 PRAK p38α  
IC50 3-12 μM 61 μM 71 μM 75 μM >100 μM  

Quality Control

Quality Control & MSDS

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Chemical structure

SC-514