CID755673

製品コードS7188 バッチS718802

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

C12H11NO3
分子量 217.22 CAS No. 521937-07-5
Solubility (25°C)* 体外 DMSO 43 mg/mL (197.95 mM)
Water Insoluble
Ethanol Insoluble
* <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 CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.
in vitro In LNCaP prostate cancer cells, CID755673 directly inhibits PKD1 activity. In HeLa cells, CID755673 significantly blocks PMA-induced nuclear export of HDAC5, and blocks PKD-mediated protein transport. In prostate cancer cells, CID755673 potently blocks cell migration and invasion, and also shows inhibition activity on tumor cell proliferation and cell cycle distribution. [1] In addition, CID755673 alter primary human NK cell effector functions. [3]
in vivo CID755673, via PKD/PKD1 inhibition, significantly ameliorates necrosis and severity of pancreatitis in a rat acute pancreatitis model. [2]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Radiometric PKD Kinase Assay
The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.
細胞アッセイ 細胞株 LNCaP or PC3 cells
濃度 ~25 μM
反応時間 6 days
実験の流れ Cell proliferation was determined by counting the number of viable cells upon trypan blue staining. Cell proliferation is measured by CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturer's instructions.
動物実験 動物モデル Rat pancreatitis model
投薬量 ~15 mg/kg
投与方法 i.p.

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：

Structural insights into regulation of the PEAK3 pseudokinase scaffold by 14-3-3 [ Nat Commun, 2023, 14(1):3543] PubMed: 37336883
FBXO28 suppresses liver cancer invasion and metastasis by promoting PKA-dependent SNAI2 degradation [ Oncogene, 2023, 42(39):2878-2891] PubMed: 37596321
FBXO28 suppresses liver cancer invasion and metastasis by promoting PKA-dependent SNAI2 degradation [ Oncogene, 2023, 10.1038/s41388-023-02809-0] PubMed: 37596321
Chemically induced revitalization of damaged hepatocytes for regenerative liver repair [ iScience, 2023, 26(12):108532] PubMed: 38144457
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710
FBXO22 Possesses Both Protumorigenic and Antimetastatic Roles in Breast Cancer Progression. [ Cancer Res, 2018, 78(18):5274-5286] PubMed: 29945959
Inhibition of protein kinase D disrupts spindle formation and actin assembly during porcine oocyte maturation. [ Aging (Albany NY), 2018, 10(12):3736-3744] PubMed: 30555056
VEGF/PKD-1 signaling mediates arteriogenic gene expression and angiogenic responses in reversible human microvascular endothelial cells with extended lifespan [Best B Mol Cell Biochem, 2018, 446(1-2):199-207] PubMed: 29380239
Klotho suppresses high phosphate-induced osteogenic responses in human aortic valve interstitial cells through inhibition of Sox9. [ J Mol Med (Berl), 2017, 95(7):739-751] PubMed: 28332126

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。