Senexin A

製品コードS8520 バッチS852001

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₁₄N₄

分子量

274.32

CAS No.

1366002-50-7

Solubility (25°C)*

体外

DMSO

54 mg/mL (196.85 mM)

Ethanol

54 mg/mL (196.85 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 1 40%PEG300 2 5%Tween80 3 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。	2.700mg/ml (9.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 54 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 adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil 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。	0.675mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	Senexin Aは、CDK8とその最も近い類縁体であるCDK19の強力かつ選択的な阻害剤であり、CDK8とCDK19のATP結合部位に対するKd値はそれぞれ0.83 μMと0.31 μMです。
in vitro	p21 is shown to activate NF-κB–dependent transcription, and Senexin A inhibits p21-stimulated activity of the consensus NF-κB–dependent promoter. This compound has no effect on p21 induction by IPTG, on cell growth with or without p21, or on p21-induced senescent phenotype. It does not affect the inhibition of gene expression by p21 and does not interfere with p21-mediated inhibition of large sets of genes belonging to Gene Ontology (GO) categories of mitosis and DNA replication. This chemical inhibits only p21-induced transcription but not other biological effects of p21. It inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. It inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. It does not inhibit ROCK and did not share cortistatin A's strong antiendothelial cell activity.
in vivo	The CDK8/19 inhibitor Senexin A reverses chemotherapy-induced paracrine tumor-promoting activities in vivo and does not inhibit reporter cell growth and showed no detectable toxicity in a mouse study.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MEF
	濃度	1 μM
	反応時間	24 h
	実験の流れ	For conditioned media mitogenic assays, MEF, untreated or treated for 24 h with 200 nM doxorubicin, alone or in combination with 1 μM Senexin A, were washed and cultured for 48 h without drugs to collect conditioned media. The media were added to A549 cells, plated on 12-well plates at 10⁴ cells per well; cells were counted after 48 h using the trypan blue exclusion assay. Experiments were performed in triplicate, and cells counted in at least three optical fields per experiment.
動物実験	動物モデル	C57BL/6 mice
	投薬量	20 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/22869755/

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：

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
P-TEFb promotes cell survival upon p53 activation by suppressing intrinsic apoptosis pathway [ Nucleic Acids Res, 2023, gkad001]	PubMed: 36727434
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer [ Breast Cancer Res, 2022, 24(1):41]	PubMed: 35715861

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。