A-205804

製品コードS2885 バッチS288501

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

C₁₅H₁₂N₂OS₂

分子量

300.4

CAS No.

251992-66-2

Solubility (25°C)*

体外

DMSO

60 mg/mL (199.73 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）

Clear solution

5%DMSO 1 Corn oil

3.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 60 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	A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.
in vitro	A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. A-205804 inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of A-205804 to inhibit PMA-induced E-selectin expression is significantly reduced (IC50 > 1000 nM), but A-205804 is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent. ^[2]

製品説明

A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.

in vitro

A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. A-205804 inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of A-205804 to inhibit PMA-induced E-selectin expression is significantly reduced (IC50 > 1000 nM), but A-205804 is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Cell ELISA Assay
キナーゼアッセイ	Primary HUVECs are plated in 96-well plates at 5 × 10⁴ cells/mL in EBM/2% FBS/human epidermal growth factor/bovine brain extract/gentamicin. The following day test compounds are added and the plates incubats for 24 h at 37 °C. TNFα then is added to a final concentration of 5 ng/mL, and the plates are incubated for an additional 6 h at 37 °C. The plates are washed once with D-PBS, and primary antibody is added in D-PBS/2% BSA /0.01% NaN3. The antibodies used are mouse monoclonal anti-ELAM-1, anti-ICAM-1, and anti-VCAM-1. The plates are stored overnight at 4 °C and then washes three times with D-PBS. Secondary antibody, HRP-conjugated donkey anti-mouse IgG in D-PBS/2%BSA, is added, and the plates are incubated for 1−2 h at room temperature and then washes three times with D-PBS. OPD solution is added to the wells, the plates are developed for 15−20 min and neutralizes with 1 N sulfuric acid, and the absorbance is read at 490 nm.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Lett, 2018, 438:105-115]

: Data from [Data independently produced by , , Acta Pharmacologica Sinica, 2018, 39: 1-12 ]

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：

Dextran sulfate prevents excess aggregation of human pluripotent stem cells in 3D culture by inhibiting ICAM1 expression coupled with down-regulating E-cadherin through activating the Wnt signaling pathway [ Stem Cell Res Ther, 2022, 13(1):218]	PubMed: 35619172
Adhesion Promotes Allergic Rhinitis CD4+IL4+ T Cell Differentiation via ICAM1 and E-Selectin [ Am J Rhinol Allergy, 2022, 19458924221086061]	PubMed: 35296145
Cathepsin D enhances breast cancer invasion and metastasis through promoting hepsin ubiquitin-proteasome degradation [Zhang C, et al. Cancer Lett, 2018, 438:105-115]	PubMed: 30227221
CTC clusters induced by heparanase enhance breast cancer metastasis [Wei RR, et al. Acta Pharmacol Sin, 2018, 39(8):1326-1337]	PubMed: 29417941
Interactions between rheumatoid arthritis synovial fibroblast migration and endothelial cells [Zimmermann-Geller B, et al. Immunol Cell Biol, 2018, 10.1111/imcb.12208]	PubMed: 30252968

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。