SD-208

製品コードS7624 バッチS762401

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

C17H10ClFN6
分子量 352.75 CAS No. 627536-09-8
Solubility (25°C)* 体外 DMSO 9 mg/mL warmed with 50ºC water bath (25.51 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 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
in vitro SD-208 inhibits the cell growth and constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity in murine SMA-560 and human LN-308 glioma cells. [1] SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro. [2] SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro. [3]
in vivo SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. [1] In syngeneic 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibits primary R3T tumor growth, and reduces the number and the size of lung metastases. [2] In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA). [3]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound.
細胞アッセイ 細胞株 Murine SMA-560 and human LN-308 glioma cells
濃度 1 μM
反応時間 48 hours
実験の流れ Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.
動物実験 動物モデル VM/Dk mice bearing SMA-560 tumors
投薬量 1 mg/mL
投与方法 p.o.

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：

Protein phosphatase PPM1A inhibition attenuates osteoarthritis via regulating TGF-β/Smad2 signaling in chondrocytes [ JCI Insight, 2023, 8(3)e166688] PubMed: 36752205
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 10.3390/cancers15205086] PubMed: 37894453
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 15(20)5086] PubMed: 37894453
Exosome-Mediated Delivery of Transforming Growth Factor-β Receptor 1 Kinase Inhibitors and Toll-Like Receptor 7/8 Agonists for Combination Therapy of Tumors [ Acta Biomater, 2022, S1742-7061(22)00004-6] PubMed: 35007784
Induction of Pro-Fibrotic CLIC4 in Dermal Fibroblasts by TGF-β/Wnt3a Is Mediated by GLI2 Upregulation [ Cells, 2022, 11(3)530] PubMed: 35159339
Berberine Suppresses Lung Metastasis of Cancer via Inhibiting Endothelial Transforming Growth Factor Beta Receptor 1 [ Front Pharmacol, 2022, 13:917827] PubMed: 35784732
TGFβ signaling is required for sclerotome resegmentation during development of the spinal column in Gallus gallus [ Dev Biol, 2022, 488:120-130] PubMed: 35644252
Loss of Yap/taz in cardiac fibroblasts attenuates adverse remodeling and improves cardiac function [ Cardiovasc Res, 2021, cvab205] PubMed: 34132780
Microphthalmia transcription factor expression contributes to bone marrow failure in Fanconi anemia. [ J Clin Invest, 2020, 130(3):1377-1391] PubMed: 31877112
Modeling Uremic Vasculopathy With Induced Pluripotent Stem Cell-Derived Endothelial Cells as a Drug Screening System [ Front Cell Dev Biol, 2020, 8:618796] PubMed: 33511129

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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