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CAS No.: 547757-23-3

BMS-345541 HCl Catalog No. CSN16421

Synonyms: BMS 345541 (hydrochloride);IKK Inhibitor III;BMS-345541

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

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技术信息

生物活性

描述NF-κB normally exists in the cytoplasm of unstimulated cells as an inactive complex with a member of the IκB inhibitory protein family. This class of protein includes IκBα, IκBβ, and IκBε. IKK-1 and IKK-2 are two catalytic subunits of IκB kinase (IKK). BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC₅₀ of 0.3 μM and 4 μM, respectively^[3]. In vitro, BMS-345541 at 0, 0.1, 1, and 10 μM treatment resulted in a concentration-dependent inhibition of melanoma cell (SK-MEL-5, A375, and Hs 294T) proliferation^[4]. In vivo, BMS-345541 (0, 10, 25, and 75 mg/kg) was administered to melanoma tumor-bearing mice orally once daily for 21 days, and it was showed that BMS-345541 effectively inhibited SK-MEL-5 tumor growth in a dose-dependent manner^[4]. BMS-345541 also dose-dependently inhibited the production of TNFα in the serum of animals challenged with an intraperitoneal administration of LPS. Approximately 50% inhibition was observed at 10 mg/kg, and dose of 100 mg/kg nearly completely inhibit serum TNFα^[3].
作用机制BMS-345541 binds to an allosteric site on IKK-2 and IKK-1.
参考文献

[1] Yang J, Amiri KI, et al. BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways. Clin Cancer Res. 2006 Feb 1;12(3Pt 1):950-60.
[2] Burke JR, Pattoli MA, et al. BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. J Biol Chem. 2003 Jan 17;278(3):1450-6.
[3] Burke JR, Pattoli MA, Gregor KR, Brassil PJ, MacMaster JF, McIntyre KW, Yang X, Iotzova VS, Clarke W, Strnad J, Qiu Y, Zusi FC. BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. J Biol Chem. 2003 Jan 17;278(3):1450-6. doi: 10.1074/jbc.M209677200. Epub 2002 Oct 25. PMID: 12403772.
[4] Yang J, Amiri KI, Burke JR, Schmid JA, Richmond A. BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways. Clin Cancer Res. 2006 Feb 1;12(3 Pt 1):950-60. doi: 10.1158/1078-0432.CCR-05-1220. PMID: 16467110; PMCID: PMC2668250.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4272 mL
- 17.1362 mL
- 34.2725 mL
- 5 mM
- 0.6854 mL
- 3.4272 mL
- 6.8545 mL
- 10 mM
- 0.3427 mL
- 1.7136 mL
- 3.4272 mL

技术信息

CAS号

547757-23-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H18ClN5

运输

蓝冰

分子量

291.78

别名

BMS 345541 (hydrochloride);IKK Inhibitor III;BMS-345541;UNII-BXU277OCN5

溶解度

DMSO	47.5 mg/mL (162.8 mM)
Water	45.0 mg/mL (154.2 mM)

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