PS 1145 dihydrochloride

Cat. No. 4569

PS 1145 dihydrochloride  [1049743-58-9]

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Chemical Name: N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride

Biological Activity

Selective IκB kinase (IKK) inhibitor (IC50 = 100 nM). Has no effect on PKA, PKC and CKII activity. Inhibits IκB-α phosphorylation and NFκB activation in HeLa cells. Inhibits NFκB-mediated proinflammatory gene expression in human airway epithelial cells. Enhances TNF-α-induced apoptosis in a multiple myeloma cell line. Attenuates LPS-induced TNF-α production in vivo. Orally active.

Technical Data

M.Wt:
395.67
Formula:
C17H11ClN4O.2HCl
Solubility:
Soluble to 5 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1049743-58-9

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Newton et al (2007) Repression of inflammatory gene expression in human pulmonary epithelial cells by small-molecule IkappaB kinase inhibitors. J.Pharmacol.Exp.Ther. 321 734. PMID: 17322026.

Castro et al (2003) Novel IKK inhibitors: beta-carbolines. Bioorg.Med.Chem.Lett. 13 2419. PMID: 12824047.

Hideshima et al (2002) NF-kappa B as a therapeutic target in multiple myeloma. J.Biol.Chem. 277 16639. PMID: 11872748.

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View Related Products by Product Action

Keywords: PS 1145 dihydrochloride, supplier, PS1145, dihydrochloride, selective, IKK, IκB, kinase, IkappaB, IKB, inhibitors, inhibits, cytokines, signaling, NFκB, NFKappaB, NFKB, TNF-alpha, TNF-a, TNF-α, orally, active, Tocris Bioscience, IκB Kinase Inhibitor products

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