ITD-1

製品コードS6713 バッチS671301

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

C27H29NO3
分子量 415.52 CAS No. 1099644-42-4
Solubility (25°C)* 体外 DMSO 83 mg/mL (199.74 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 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.
in vitro

ITD-1, a small molecule inhibitor of TGF-β signaling, can partially induce proteasomal degradation of the TβR232,33, and blocks Smad and MAPK activation.[2]
in vivo

ITD-1 partially inhibits TGF-β signaling and renal fibrosis in unilateral ischemia-reperfusion injury (UIRI) mice.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NRK-49F cells
濃度 3 μM
反応時間 1 h
実験の流れ

NRK-49F cells are pre-incubated with KP1 (10 µg/ml, 3 μM) or ITD-1 (3 μM) for 1 h, and then treated with TGF-β1 (2 ng/ml) for 45 min. Western blot analyses the protein levels of p-Smad3 and p-p38.
動物実験 動物モデル unilateral ischemia-reperfusion injury (UIRI) mice, unilateral ureter obstruction (UUO) mice
投薬量 0.31 μM/kg
投与方法 IOCV

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：

Alpha-hederin reprograms multi-miRNAs activity and overcome small extracellular vesicles-mediated paclitaxel resistance in NSCLC [ Front Pharmacol, 2024, 15:1257941] PubMed: 38362150
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A Klotho-derived peptide protects against kidney fibrosis by targeting TGF-β signaling [ Nat Commun, 2022, 13(1):438] PubMed: 35064106
TGF-β induces GBM mesenchymal transition through upregulation of CLDN4 and nuclear translocation to activate TNF-α/NF-κB signal pathway [ Cell Death Dis, 2022, 13(4):339] PubMed: 35418179
HOXA10 mediates epithelial-mesenchymal transition to promote gastric cancer metastasis partly via modulation of TGFB2/Smad/METTL3 signaling axis [ J Exp Clin Cancer Res, 2021, 40(1):62] PubMed: 33563300
Discovery of a novel short peptide with efficacy in accelerating the healing of skin wounds [ Pharmacol Res, 2020, S1043-6618(20)31604-2] PubMed: 33220421
Human induced pluripotent stem cell-derived cardiomyocytes reveal abnormal TGFβ signaling in type 2 diabetes mellitus. [ J Mol Cell Cardiol, 2020, 3;142:53-64] PubMed: 32251671
Transforming growth factor-β1 suppress pentraxin-3 in human orbital fibroblasts. [ Endocrine, 2020, 16] PubMed: 32300954
Activation of E-prostanoid 3 receptor in macrophages facilitates cardiac healing after myocardial infarction. [ Nat Commun, 2017, 8:14656] PubMed: 28256515

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