TP0427736 HCl

製品コードS8700 バッチS870001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C14H11ClN4S2
分子量 334.85 CAS No. 864374-00-5
Solubility (25°C)* 体外 DMSO 67 mg/mL (200.08 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.

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生物活性

製品説明 TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.
in vitro

TP0427736 inhibits Smad2/3 phosphorylation in a concentration-dependent manner, with an IC50 value of 8.68 nM. In a cell-based assay of outer root sheath cells, TP0427736 rescued the inhibited proliferation by TGF-β1 and TGF-β2 in a concentration-dependent manner[1].
in vivo

TP0427736 decreases shortening of hair follicle length during the transition from the late anagen phase to the catagen phase[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 A549 cells
濃度 --
反応時間 2 h
実験の流れ

A549 cells are cultured in plates overnight at 37℃ in a 5% CO2, 95% air atmosphere. Cells are pretreated with various concentrations of TP0427736 or DMSO as a control for 2 h, followed by the addition of 1 ng/mL TGF-β1. After 1 h of incubation, the cells are washed with PBS and lysed with RIPA solution, then mixed with biotinylated anti-Smad2/3 antibody. The mixture is transferred to a streptavidin-coated 96 well plate and incubated for 2 h. The mixture is then discarded, and each well is treated with rabbit anti-phosphoserine antibody, followed by Eu-labeled anti-rabbit IgG antibody and DELFIA Enhancement solution. The developed fluorescence is measured using an ARVO multi-label counter. The IC50 values are determined by analyzing the concentration-response curves.

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：

Bmp8a deletion leads to obesity through regulation of lipid metabolism and adipocyte differentiation [ Commun Biol, 2023, 6(1):824] PubMed: 37553521
BMP8B Activates Both SMAD2/3 and NF-κB Signals to Inhibit the Differentiation of 3T3-L1 Preadipocytes into Mature Adipocytes [ Nutrients, 2023, 16(1)64] PubMed: 38201894
Bmp4 in Zebrafish Enhances Antiviral Innate Immunity through p38 MAPK -Mitogen-Activated Protein Kinases) Pathway [ Int J Mol Sci, 2023, 24(19)14444] PubMed: 37833891
Bmp8a is an essential positive regulator of antiviral immunity in zebrafish [ Commun Biol, 2021, 4(1):318] PubMed: 33750893
A novel tsRNA-16902 regulating the adipogenic differentiation of human bone marrow mesenchymal stem cells [ Stem Cell Res Ther, 2020, 11(1):365] PubMed: 32831139
Regulatory mechanism of NOV/CCN3 in the inflammation and apoptosis of lung epithelial alveolar cells upon lipopolysaccharide stimulation. [ Mol Med Rep, 2019, 10.3892/mmr.2019.10655] PubMed: 31545412

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。

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