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Inhibitor SourceBook™ Second Edition

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Other <strong>Inhibitor</strong>s of Biological Interest<br />

NF-kB Activation <strong>Inhibitor</strong>s<br />

Product Cat. No. Comments Size Price<br />

BAY -7082 196870 {(E)3-[(4-Methylphenyl)sulfonyl]-2-propenenitrile}<br />

Potential anti-inflammatory agent that selectively and irreversibly<br />

inhibits the TNFa-inducible phosphorylation of IkBa (IC 50 = 0 mM)<br />

without affecting the constitutive IkBa phosphorylation. Decreases<br />

nuclear translocation of NF-kB and inhibits TNFa-induced surface<br />

expression of the endothelial-leukocyte cell adhesion molecules<br />

E-selectin, VCAM- , and ICAM- .<br />

N InSolution BAY -7082 196871 A 00 mM ( 0 mg/483 ml) solution of BAY -7082<br />

(Cat. No. 96870) in DMSO.<br />

BAY -7085 196872 {(E)3-[(4-t-Butylphenyl)sulfonyl]-2-propenenitrile}<br />

Exhibits biological properties similar to that of BAY -7082<br />

(Cat. No. 96870). BAY -7085 has also been shown to have potent<br />

anti-inflammatory properties in vivo.<br />

CAPE 211200 (Caffeic Acid Phenethyl Ester, Synthetic)<br />

An active component of propolis from honeybee hives with antiviral,<br />

anti-inflammatory, and immunomodulatory properties. Has been<br />

shown to act as a potent and specific inhibitor of NF-kB activation.<br />

(E)-Capsaicin 211274 {[(E)-N-(4-Hydroxy-3-methoxyphenyl)methyl]-8-methyl-6nonenamide}<br />

An active constituent of cayenne pepper that has anti-nociceptive<br />

and anti-inflammatory effects. Inhibits NF-kB activation by TNF-a.<br />

N Evodiamine, Evodia rutaecarpa 341211 A cell-permeable quinazolinocarboline that suppresses both<br />

inducible and constitutive NF-kB activation and<br />

NF-kB-regulated gene expression by inhibiting IKK activation.<br />

Gliotoxin, Gladiocladium<br />

fimbriatum<br />

Helenalin, A. chamissonis ssp.<br />

foliosa<br />

371715 {2,3,5a,6-Tetrahydro-6-hydroxy-3(hyroxymethyl)-2-methyl-10H-<br />

3a,10a-epidithio-pyrazinol[1,2a]indole-1,4-dione}<br />

An immunosuppressive secondary metabolite produced by several<br />

pathogenic fungi that specifically inhibits NF-kB activation in B and<br />

T cells at nanomolar concentrations.<br />

374000 A cell-permeable pseudoguainolide sesquiterpenoid lactone that<br />

inhibits NF-kB-DNA binding activity by selectively alkylating the p65<br />

subunit of NF-kB. Does not inhibit IkB degradation or NF-kB nuclear<br />

translocation.<br />

Hypoestoxide, Hypoestes rosea 401006 A naturally occurring, cell-permeable diterpene with antiinflammatory<br />

properties. Acts as a selective and direct inhibitor of<br />

IkB kinase (IC 50 = 24 mM) in TNF-a stimulated HeLa cells thereby<br />

prevents NF-kB activation.<br />

IkB Kinase <strong>Inhibitor</strong> Peptide,<br />

Cell-Permeable<br />

IkB Kinase Inactive Control<br />

Peptide, Cell-Permeable<br />

401477 (Ac-AAVALLPAVLLALLAPDDRHDSGLDSMKDE-NH 2 )<br />

A 4-amino acid peptide corresponding to the active IkB<br />

phosphorylation recognition sequence, linked to the hydrophobic<br />

region of the fibroblast growth factor signal peptide to aid in cellular<br />

delivery. Specifically inhibits LPS-induced IkB degradation by IkB<br />

kinases (IKK) in RAW 264.7 cells ( 0 mM) or TNF-a production<br />

(IC 50 > 0 mM).<br />

401478 (Ac-AAVALLPAVLLALLAPDDRHDAGLDAMKDE-NH 2 )<br />

An inactive control for IkB Kinase <strong>Inhibitor</strong> Peptide (Cat. No.<br />

40 477). Corresponds to the mutated recognition sequence of IkB<br />

(Ser 32 → Ala and Ser 36 → Ala), linked to the hydrophobic region of<br />

the fibroblast growth factor signal peptide to aid in cellular delivery.<br />

Does not have any inhibitory effect on LPS-induced IkB degradation<br />

by IkB kinases (IKK) in RAW 264.7 cells at 50 mg/ml.<br />

IKK <strong>Inhibitor</strong> II, Wedelolactone 401474 (7-Methoxy-5,11,12-trihydroxy-coumestan; Wedelolactone, Eclipta alba)<br />

The naturally isolated active ingredient of the herbal medicine,<br />

Eclipta alba, that acts as a selective and irreversible inhibitor of IKKa<br />

and b kinase activity (IC 50 < 0 mM). Inhibits NF-kB-mediated gene<br />

transcription in cells by blocking the phosphorylation and degradation<br />

of IkB.<br />

0 mg $68<br />

0 mg $68<br />

0 mg $88<br />

25 mg $ 00<br />

00 mg $62<br />

5 mg $ 49<br />

mg $8<br />

500 mg $ 35<br />

mg $ 50<br />

mg $ 90<br />

54 Orders Phone 800 854 34 7<br />

Calbiochem • <strong>Inhibitor</strong> SourceBook<br />

Fax 800 776 0999<br />

Web www.emdbiosciences.com/calbiochem<br />

mg<br />

mg<br />

$ 95<br />

$79

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