PS-1145

製品コードS7691 バッチS769101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H11ClN4O
分子量 322.75 CAS No. 431898-65-6
Solubility (25°C)* 体外 DMSO 64 mg/mL (198.29 mM)
Ethanol (warmed with 50ºC water bath) 2 mg/mL (6.19 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.07mg/ml Taking the 1 mL working solution as an example, add 50 μL of 21.3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
in vitro

PS-1145 blocks TNFalpha-induced NF-kappaB activation through inhibition of IkappaBalpha phosphorylation, and blocks the protective effect of IL-6 against Dex-induced apotosis. PS-1145 also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. [1] In human primary CD4(+) T cells, PS-1145 abrogates cell proliferation and impairs the activation of NF-κB and AP-1 transcription factors by engagement of CD3 and CD28 coreceptor. [2]
in vivo

In male Wistar rats with 7,12-dimethylbenz[α]anthracene-induced skin tumor, PS-1145 (50 mg/kg, i.v.) enhances tumor cell apoptosis by up-regulating p53, activating caspases and down regulating NF-κB and VEGF factor, and thus induces the tumor progression. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
PS-1145 are dissolved in DMSO and stored at −20 °C until use. Ki value of PS-1145 against the IKK complex is determined by measuring Km , ATP against varying fixed concentration of the inhibitor. Briefly, partially purified IKK complex obtained from unstimulated HeLa S3 cells are pre-activated using the catalytic domain of MEKK1 expressed in sf9. Kinase activity is assessed using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km ,peptide = 30 μM,K m , ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies in an ELISA format with appropriate standard curve for quantification. For PS-1145 Ki measurement, the activated IKK complex is first preincubated in varying fixed concentration of the inhibitor (0.1–1 μM) at 25 °C for 1 h. Then apparentK m measurement for MgATP is performed at each discrete inhibitor concentration.
細胞アッセイ 細胞株 MM.1S, U266, and RPMI8226 cell lines
濃度 ~50 μM
反応時間 48 h
実験の流れ

The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer.
動物実験 動物モデル Male Wistar rats with 7,12-dimethylbenz[α]anthracene-induced skin tumor
投薬量 ~50 mg/kg
投与方法 i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Redox Biol, 2017, 562-576]

Data from [Data independently produced by , , J Biol Chem, 2018, 293(19):7268-7280]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses [ Cell Chem Biol, 2022, 29(7):1113-1125.e6] PubMed: 35728599
TRAF-interacting protein with forkhead-associated domain (TIFA) transduces DNA damage-induced activation of NF-κB [Fu J J Biol Chem, 2018, 293(19):7268-7280] PubMed: 29581234
Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. [Tse AK, et al. Redox Biol, 2017, 562-576] PubMed: 28107677
Pathogenic role of B-cell receptor signaling and canonical NF-κB activation in mantle cell lymphoma. [ Blood, 2016, 128(1):82-92] PubMed: 27127301

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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