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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.070mg/ml (3.32mM) 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. This compound also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. [1] In human primary CD4(+) T cells, it 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 this compound 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 this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11872748/
  • https://pubmed.ncbi.nlm.nih.gov/22331067/
  • https://pubmed.ncbi.nlm.nih.gov/26148342/

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。