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Submit ReviewBMS 345541 is a 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.
BMS 345541 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 291.78 |
公式 | C14H17N5.HCl |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 29.18 | 100 | |
DMSO | 29.18 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for BMS 345541, please let us know.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 BMS 345541 的部分引用包括:
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
Michael et al (2019) Interleukin-1β Induces mtDNA Release to Activate Innate Immune Signaling via cGAS-STING. Mol Cell 74 801-815.e6 PMID: 30952515
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BMS 345541 was added to pancreatic acinar 3-dimensional cultures and differentiation of the cultures was monitored for 3 to 4 days. The concentration ranged between 1 and 10 uM.