Home NF-κB IκB/IKK inhibitor SC-514 For research use only.

SC-514

Synonyms: GK 01140

SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

SC-514 Chemical Structure

SC-514 Chemical Structure

CAS No. 354812-17-2

Purity & Quality Control

Batch: S490701 DMSO]45 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
99.9

SC-514 Related Products

Signaling Pathway

IκB/IKK Signaling Pathways

IκB/IKK Signaling Pathway

Biological Activity

Description SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
Targets
IKK2 [1] CDK2/CyclinA [1] AUR2 [1] PRAK [1] MSK [1]
3 μM-12 μM 61 μM 71 μM 75 μM 123 μM
In vitro
In vitro 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-κB-dependent IL-6, IL-8, and COX-2 genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts (RASFs) with IC50s of 20, 20 and 8 μM. 100 μM SC-514 blocks the phosphorylation and degradation of IκBα and also reduces the level of translocation of p65 into the nucleus in IL-1β-treated RASFs SC-514 does not inhibit the phosphorylation and activation of the IKK complex. SC-514 induces a delay but not a complete blockade in IκBα phosphorylation and degradation. SC-514 treatment cells shows a slightly slowed, decreased import of p65 into the nucleus and a faster export of p65 from the nucleus. SC-514 inhibits the phosphorylation of either IκBα or p65 similarly. [1]
In Vivo
In vivo SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNF-α production. SC-514 (50 mg/kg, i.p.) inhibits TNF-αproduction in vivo by ~70%. [1]

Chemical Information & Solubility

Molecular Weight 224.3 Formula

C9H8N2OS2
CAS No. 354812-17-2 SDF Download SC-514 SDF
Smiles C1=CSC=C1C2=CC(=C(S2)C(=O)N)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (200.62 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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