SC 514

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Cat.No. 3318 - SC 514 | C9H8N2OS2 | CAS No. 354812-17-2
Description: IKKβ inhibitor; attenuates NF-κB-induced gene expression
Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Orally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 μM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 μM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.

Licensing Information

Sold for research purposes under agreement from AstraZeneca

Technical Data

M. Wt 224.3
Formula C9H8N2OS2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 354812-17-2
PubChem ID 2807869
InChI Key BMUACLADCKCNKZ-UHFFFAOYSA-N
Smiles NC1=C(C(N)=O)SC(C2=CSC=C2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.43 100
ethanol 2.24 10

Preparing Stock Solutions

The following data is based on the product molecular weight 224.3. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.46 mL 22.29 mL 44.58 mL
5 mM 0.89 mL 4.46 mL 8.92 mL
10 mM 0.45 mL 2.23 mL 4.46 mL
50 mM 0.09 mL 0.45 mL 0.89 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kishore et al (2003) A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts. J.Biol.Chem. 278 32861 PMID: 12813046

Gomez et al (2005) Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br.J.Pharmacol. 146 217 PMID: 15997236

Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817 PMID:


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Keywords: IKK-2 inhibitors inhibits attenuates NF-κB NF-kappaB-induced gene expression NF-kB IKK IκB IkappaB Kinases Nuclear Factor Kappa B NF-kappaB Cytokine Signaling Signalling Transcription Factors SC514 AstraZeneca IkB Kinase

1 Citation for SC 514

Citations are publications that use Tocris products. Selected citations for SC 514 include:

Akhtar et al (2015) MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes. Nature 67 423 PMID: 25385442


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