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PS 1145 dihydrochloride

Catalog #: 4569
4 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4569/10
4569/50
PS 1145 dihydrochloride | CAS No. 1049743-58-9 | IkB Kinase Inhibitors
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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%

Product Details
Citations (4)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

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

Background References

  1. Novel IKK inhibitors: beta-carbolines.
    Castro et al.
    Bioorg.Med.Chem.Lett., 2003;13:2419
  2. Repression of inflammatory gene expression in human pulmonary epithelial cells by small-molecule IkappaB kinase inhibitors.
    Newton et al.
    J.Pharmacol.Exp.Ther., 2007;321:734
  3. NF-kappa B as a therapeutic target in multiple myeloma.
    Hideshima et al.
    J.Biol.Chem., 2002;277:16639

Product Datasheets

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Citations for PS 1145 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for PS 1145 dihydrochloride include:

4 Citations: Showing 1 - 4

  1. NF-κB memory coordinates transcriptional responses to dynamic inflammatory stimuli.
    Authors: Savas Et al.
    Cell Rep  2022;40:111159
  2. Induction of IDO1 and Kynurenine by Serine Proteases Subtilisin, Prostate Specific Antigen, CD26 and HtrA: A New Form of Immunosuppression?
    Authors: L Gail Et al.
    Front Immunol  2022;13:832989
  3. The cell polarity kinase Par1b/MARK2 activation selects specific NF-kB transcripts via phosphorylation of core mediator Med17/TRAP80.
    Authors: Anastasia Et al.
    Mol Biol Cell  2021;32:690-702
  4. Loss of the oncogenic phosphatase PRL-3 promotes a TNF-R1 feedback loop that mediates triple-negative breast cancer growth.
    Authors: Gari Et al.
    Oncogenesis  2016;5:e255

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