401489
IKK Inhibitor X - CAS 431898-65-6 - Calbiochem
Synonym(s):
N-(6-Chloro-9H-β-carbolin-8-yl)nicotinamide, PS-1145
assay
≥98% (HPLC)
form
solid
color
yellow
solubility
DMSO: 50 mg/mL
General description
A cell-permeable β-carboline compound that displays anti-inflammatory properties. Acts as a potent, ATP-competitive, and reversible inhibitor of IKK (IC50 = 88 nM) with selectivity over 14 other commonly studied kinases (IC50 >100 μM), including NF-κB inducing kinase. Blocks cellular IκBα phosphorylation and NF-κB activation (EC50 = 5 μM in TNF-α-treated HeLa cells) in vitro and reduces TNF-α release in plasma of LPS-challenged mice in vivo (50 mg/ml, p.o.).
The IKK Inhibitor X controls the biological activity of IKK. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.
Biochem/physiol Actions
Target IC50:88 nM against IKK
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Storage Class
10-13 - German Storage Class 10 to 13
Regulatory Information
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Alfredo C Castro et al.
Bioorganic & medicinal chemistry letters, 13(14), 2419-2422 (2003-06-26)
Inhibitors of IkappaB kinase (IKK) have long been sought as specific regulators of NF-kappaB. A screening effort of the endogenous IKK complex allowed us to identify 5-bromo-6-methoxy-beta-carboline as a nonspecific IKK inhibitor. Optimization of this beta-carboline natural product derivative resulted
Danyi Wen et al.
The Journal of pharmacology and experimental therapeutics, 317(3), 989-1001 (2006-03-10)
IkappaB kinase (IKK) beta is essential for inflammatory cytokine-induced activation of nuclear factor kappaB (NF-kappaB). NF-kappaB plays a pivotal role in the function of major cell types that contribute to the pathophysiological process of rheumatoid arthritis (RA). Here, we report
Matthew C Catley et al.
Molecular pharmacology, 70(2), 697-705 (2006-05-12)
Asthma and chronic obstructive pulmonary disease (COPD) are characterized by chronic airway inflammation. However, because patients with COPD and certain patients with asthma show little or no therapeutic benefit from existing corticosteroid therapies, there is an urgent need for novel
Teru Hideshima et al.
The Journal of biological chemistry, 277(19), 16639-16647 (2002-03-02)
We have shown that thalidomide (Thal) and its immunomodulatory derivatives (IMiDs), proteasome inhibitor PS-341, and As(2)O(3) act directly on multiple myeloma (MM) cells and in the bone marrow (BM) milieu to overcome drug resistance. Although Thal/IMiDs, PS-341, and As(2)O(3) inhibit
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