PS 1145 dihydrochloride

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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)
Citations (4)

Biological Activity for PS 1145 dihydrochloride

PS 1145 dihydrochloride is a 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 for PS 1145 dihydrochloride

M. Wt 395.67
Formula C17H11ClN4O.2HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1049743-58-9
PubChem ID 16219884
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PS 1145 dihydrochloride

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

Preparing Stock Solutions for PS 1145 dihydrochloride

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

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for PS 1145 dihydrochloride

References for PS 1145 dihydrochloride

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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4 Citations for PS 1145 dihydrochloride

Citations are publications that use Tocris products. Selected citations for PS 1145 dihydrochloride include:

Anastasia et al (2021) The cell polarity kinase Par1b/MARK2 activation selects specific NF-kB transcripts via phosphorylation of core mediator Med17/TRAP80. Mol Biol Cell 32 690-702 PMID: 33596087

Savas et al (2022) NF-κB memory coordinates transcriptional responses to dynamic inflammatory stimuli. Cell Rep 40 111159 PMID: 35977475

L Gail et al (2022) Induction of IDO1 and Kynurenine by Serine Proteases Subtilisin, Prostate Specific Antigen, CD26 and HtrA: A New Form of Immunosuppression? Front Immunol 13 832989 PMID: 35371018

Gari et al (2016) Loss of the oncogenic phosphatase PRL-3 promotes a TNF-R1 feedback loop that mediates triple-negative breast cancer growth. Oncogenesis 5 e255 PMID: 27526109

Do you know of a great paper that uses PS 1145 dihydrochloride from Tocris? Please let us know.

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