[CAS NO. 354812-17-2] SC-514

Name: SC-514
Brand: Arctom Scientific
SKU: SLK-S4907

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PRODUCTS SPECIFICATIONS [354812-17-2]

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Catalog

SLK-S4907

Brand

Selleck

CAS

354812-17-2

DESCRIPTION [354812-17-2]

Overview

MDL	MFCD00206459
Molecular Weight	224.3
Molecular Formula	C9H8N2OS2
SMILES	C(N)(=O)C=1SC(=CC1N)C=2C=CSC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	4.4583 mL	22.2916 mL	44.5831 mL
5 mM	0.8917 mL	4.4583 mL	8.9166 mL
10 mM	0.4458 mL	2.2292 mL	4.4583 mL
50 mM	0.0892 mL	0.4458 mL	0.8917 mL

Description

SC-514 (GK 01140) is an orally active, ATP-competitive inhibitor with of 3-12 μM, blocks -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

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.

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%.

References

[1] Kishore N, et al. J Biol Chem, 2003, 278(35), 32861-32871.

Synonyms

[2,3′-Bithiophene]-5-carboxamide, 4-amino-

4-Amino[2,3′-bithiophene]-5-carboxamide

4-Amino-[2,3′]bithiophenyl-5-carboxamide

3-Amino-5-(3-thienyl)thiophene-2-carboxamide

SC 514

GK 01140

3-Amino-5-thiophen-3-ylthiophene-2-carboxamide

3-Amino-5-(thiophen-3-yl)thiophene-2-carboxamide