Catalog Number: 4899
Chemical Name: N-(6-Chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide dihydrochloride
Biological Activity
Novel, ATP-competitive IKK2-selective inhibitor (IC50 = 60 nM at 50 μM ATP). Exhibits no inhibition at IKK1 (EC50 >100 μM), IKKε (EC50 >100 μM) or a panel of 28 other kinases (EC50 >50 μM). Exhibits antitumor activity in lymphoma-bearing SCID mice. Demonstrates synergistic cytotoxic effects with vincristine (Cat. No. 1257).
Technical Data
  • M.Wt:
    439.72
  • Formula:
    C19H15ClN4O2.2HCl
  • Solubility:
    Soluble to 20 mM in DMSO and to 5 mM in water with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at +4°C
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.
Background References
  1. Validation of the anti-inflammatory properties of small-molecule IkappaB Kinase (IKK)-2 inhibitors by comparison with adenoviral-mediated delivery of dominant-negative IKK1 and IKK2 in human airways smooth muscle.
    Catley et al.
    Mol.Pharmacol., 2006;70:697
  2. Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta.
    Nagashima et al.
    Blood, 2006;107:4266
  3. I-kappa-kinase-2 (IKK-2) inhibition potentiates vincristine cytotoxicity in non-Hodgkin's lymphoma.
    Al-Katib et al.
    Mol.Cancer, 2010;9:1476

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