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Submit ReviewBMS 345541
Description: Selective allosteric inhibitor of IKK; anti-inflammatory
Chemical Name: N1-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Selective allosteric inhibitor of IKK (IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively). Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. Also suppresses joint destruction in a mouse model of arthritis.
Compound Libraries
BMS 345541 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 291.78 |
| Formula | C14H17N5.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 547757-23-3 |
| PubChem ID | 9926054 |
| InChI Key | MIDKPVLYXNLFGZ-UHFFFAOYSA-N |
| Smiles | NCCNC1=NC3=C(C=C(C)C=C3)N2C1=NC=C2C.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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 29.18 | 100 | |
| DMSO | 29.18 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 291.78. 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 |
|---|---|---|---|
| 1 mM | 3.43 mL | 17.14 mL | 34.27 mL |
| 5 mM | 0.69 mL | 3.43 mL | 6.85 mL |
| 10 mM | 0.34 mL | 1.71 mL | 3.43 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.69 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Pattoli et al (2005) Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression. J.Pharmacol.Exp.Ther. 315 382 PMID: 16009742
Burke et al (2003) BMS-345541 is a highly selective inhibitor of IκB kinase that binds at an allosteric site of the enzyme and blocks NF- κB-dependent transcription in mice. J.Biol.Chem. 278 1450 PMID: 12403772
De Silva et al (2010) Inhibition of choriodecidual cytokine production and inflammatory gene expression by selective IκB kinase (IKK) inhibitors. Br.J.Pharmacol. 160 1808 PMID: 20649582
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Keywords: BMS 345541, BMS 345541 supplier, BMS345541, Selective, IKK, allosteric, inhibitors, inhibits, anti-inflammatory, IKKβ, IKKμ, arthritis, IKK1, IKK2, IkB, Kinase, NF-kB/IkB, 4806, Tocris Bioscience
1 Citation for BMS 345541
Citations are publications that use Tocris products. Selected citations for BMS 345541 include:
Reho et al (2019) Mechanistic Target of Rapamycin Complex 1 Signaling Modulates Vascular Endothelial Function Through Reactive Oxygen Species. J Am Heart Assoc 8 e010662 PMID: 31020916
Do you know of a great paper that uses BMS 345541 from Tocris? Please let us know.
Reviews for BMS 345541
Average Rating: 5 (Based on 1 Review.)
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Great, easy to store.
By
Brian Englar on 02/06/2019
Assay Type: Ex Vivo
Species: Human
Cell Line/Tissue: MDA-231
This IKK inhibitor worked in our evaluation of TAK1 in MDA-231 cells. We compared the ability of this inhibitor to induce TNf mediated death to a TAK1 inhibitor.
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