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SC-514

Cayman Chemical Item Number 10010267

(CAS 354812-17-2)

SC-514 (CAS 354812-17-2)

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Description

SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.1,2 In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).1 SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells3 and TLR2 in TNF-activated astrocytes.4

1 Kishore, N., Sommers, C., Mathialagan, S., et al. A selective IKK-2 inhibitor blocks NF-kB-dependent gene expression in interleukin-1b-stimulated synovial fibroblasts. J Biol Chem 278(35) 32861-32871 (2003).

2 Baxter, A., Brough, S., Cooper, A., et al. Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorg Med Chem Lett 14 2817-2822 (2004).

3 Gomez, A.B., MacKenzie, C., Paul, A., et al. Selective inhibition of inhibitory kappa B kinase-b abrogates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br J Pharmacol 146 217-225 (2005).

4 Phulwani, N.K., Esen, N., Syed, M.M., et al. TLR2 expression in astrocytes is induced by TNF-a-and NF-kB-dependent pathways. J Immunol 181 3841-3849 (2008).

Formal Name 4-​amino-​[2,​3'-​bithiophene]-​5-​carboxamide
CAS Number 354812-17-2
Molecular Formula C9H8N2OS2
Formula Weight 224.3
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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NC(=O)​c1sc(cc1N)​c1cscc1

Background Reading

Phulwani, N.K., Esen, N., Syed, M.M., et al. TLR2 expression in astrocytes is induced by TNF-a-and NF-kB-dependent pathways. J Immunol 181 3841-3849 (2008).

Gomez, A.B., MacKenzie, C., Paul, A., et al. Selective inhibition of inhibitory kappa B kinase-b abrogates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br J Pharmacol 146 217-225 (2005).

Baxter, A., Brough, S., Cooper, A., et al. Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorg Med Chem Lett 14 2817-2822 (2004).

Kishore, N., Sommers, C., Mathialagan, S., et al. A selective IKK-2 inhibitor blocks NF-kB-dependent gene expression in interleukin-1b-stimulated synovial fibroblasts. J Biol Chem 278(35) 32861-32871 (2003).

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Size Price Quantity Subtotal
5 mg $35.00 $0.00
10 mg $67.00 $0.00
25 mg $158.00 $0.00
50 mg $280.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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