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 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| PubChem ID | 90488985 |
| InChI Key | AWKOVWFBTRXQLW-UHFFFAOYSA-N |
| Smiles | ClC1=C(OC)C(NC(C4=CC=CN=C4C)=O)=C2C(C(C=CN=C3)=C3N2)=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 | 8.79 | 20 | |
| water | 2.2 | 5mM 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.37 mL | 22.74 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.55 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: ML 120B dihydrochloride, supplier, ML120B, dihydrochloride, IKK2, inhibitor, ikk-2, NF-kappaB, NF-kB, NF-κ, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, potent, selective, inhibitors, inhibits, inhibitory, factor-kappab, αb, kinases, NF-kB/IkB, IkB, Kinase, IkB, Kinase, Tocris Bioscience
