PS 1145 dihydrochloride

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Cat.No. 4569 - PS 1145 dihydrochloride | CAS No. 1049743-58-9
Description: Selective IKK inhibitor; orally active
Chemical Name: N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1049743-58-9
PubChem ID 16219884
InChI Key QTDCBADLGJZBHP-UHFFFAOYSA-N
Smiles ClC1=CC(NC(C4=CC=CN=C4)=O)=C(NC3=C2C=CN=C3)C2=C1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 1.98 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 395.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 50.55 mL 252.74 mL 505.47 mL
0.25 mM 10.11 mL 50.55 mL 101.09 mL
0.5 mM 5.05 mL 25.27 mL 50.55 mL
2.5 mM 1.01 mL 5.05 mL 10.11 mL

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References

References are publications that support the biological activity of the product.

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

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

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 all IκB Kinase Inhibitors

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