WM-1119

製品コードS8776 バッチS877601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₈H₁₃F₂N₃O₃S

分子量

389.38

CAS No.

2055397-28-7

Solubility (25°C)*

体外

DMSO

78 mg/mL (200.31 mM)

Water

Insoluble

Ethanol

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 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。	5.000mg/ml (12.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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.
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。	5.000mg/ml (12.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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.

* <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	WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively.
in vitro	Treatment of MEFs with WM-1119 resulted in cell cycle arrest in G1 and a senescence phenotype. Treatment with this compound inhibits the proliferation of the EMRK1184 lymphoma cells in vitro. This treatment results in increased levels of Cdkn2a and Cdkn2b mRNA and p16^INK4a and p19^ARF proteins, as well as a delayed increase in Cdkn1a mRNA^[1].
in vivo	WM-1119 is effective in treating lymphoma in vivo while its treatment has no effect on haematocrit, erythrocytes or platelet numbers, but there was overall leukopenia^[1].

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/30069049/

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：

MOZ and Menin-MLL Complexes are Complementary Regulators of Chromatin Association and Transcriptional Output in Gastrointestinal Stromal Tumor [ Cancer Discov, 2022, candisc.0646.2021]	PubMed: 35499757
KAT6A, a novel regulator of β-catenin, promotes tumorigenicity and chemoresistance in ovarian cancer by acetylating COP1 [ Theranostics, 2021, 11(13):6278-6292]	PubMed: 33995658
KAT6A is associated with sorafenib resistance and contributes to progression of hepatocellular carcinoma by targeting YAP [ Biochem Biophys Res Commun, 2021, 585:185-190]	PubMed: 34808502
Lysine acetylation participates in boar spermatozoa motility and acrosome status regulation under different glucose conditions [ Theriogenology, 2021, 159:140-146]	PubMed: 33152539
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model [ J Med Chem, 2020, 31]	PubMed: 32191458

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。