ML 120B dihydrochloride
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).
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||2.2||5 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 439.72. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||11.37 mL||56.85 mL||113.71 mL|
|1 mM||2.27 mL||11.37 mL||22.74 mL|
|2 mM||1.14 mL||5.69 mL||11.37 mL|
|10 mM||0.23 mL||1.14 mL||2.27 mL|
References are publications that support the biological activity of the product.
Catley et al (2006) 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. Mol.Pharmacol. 70 697 PMID: 16687566
Nagashima et al (2006) Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta. Blood 107 4266 PMID: 16439676
Al-Katib et al (2010) I-kappa-kinase-2 (IKK-2) inhibition potentiates vincristine cytotoxicity in non-Hodgkin's lymphoma. Mol.Cancer 9 1476 PMID: 20809973
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RAW macrophages were incubated with 1 μM ML 120B for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with ML 120B.
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