RepSox (E-616452)

製品コードS7223 バッチS722305

印刷

化学情報

Chemical Structure Synonyms SJN 2511,ALK5 Inhibitor II Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H13N5
分子量 287.32 CAS No. 446859-33-2
Solubility (25°C)* 体外 DMSO 57 mg/mL (198.38 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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.
in vitro

RepSox (E-616452) inhibits ATP binding to ALK5 and ALK5 autophosphorylation with IC50 of 23 nM and 4 nM, respectively. It also inhibits TGF-β induced cellular PAI-1 luciferase activity with IC50 of 18 nM. [1]

This compound is able to successfully replace Sox2 in reprogramming by inhibiting transforming growth factor-β (Tgf-β) signaling, which in turn induces Nanog expression. Effect of RepSox inducing reprogramming does not require chromatin remodeling. It is found to be efficient at generating iPSCs. [2]
in vivo

When injected into blastocysts, RepSox (E-616452) is able to contribute to forming chimeric embryos in vivo. A one-day treatment with this compound is sufficient to replace transgenic Sox2. [2]

プロトコル(参考用のみ)

キナーゼアッセイ ALK5 fluorescence polarization binding assay
Compound binding to ALK5 is tested on purified recombinant GST- ALK5 (residues 198-503). Displacement of rhodamine green fluorescently labeled ATP competitive inhibitor by different concentrations of test compounds is used to calculate a binding pIC50. GST -ALK5 is added to a buffer containing 62.5 mM Hepes, pH 7.5, 1 mM DTT, 12.5 mM MgCl2, 1.25 mM CHAPS, and 1 nM rhodamine green-labeled ligand so that the final ALK5 concentration is 10 nM based on active site titration of the enzyme. Forty microliters of the enzyme/ligand reagent is added to 384 well assay plates containing 1 μL of different concentrations of RepSox (E-616452). This compound is used to construct concentration-response curves. The plates are read immediately on a fluorescence reader with excitation, emission, and dichroic filters of 485, 530, and 505 nm, respectively. The fluorescence polarization for each well is calculated by the Acquest and is then imported into curve fitting software.
細胞アッセイ 細胞株 BxPC-3 cells
濃度
反応時間 24 h
実験の流れ

Before adding TGF-β, cells were treated with RepSox (E-616452) for 24 hours.
動物実験 動物モデル Male C57BL/6 mice
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15317461/
  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3335195/
  • https://pubmed.ncbi.nlm.nih.gov/36207615/
  • https://pubmed.ncbi.nlm.nih.gov/32066676/

カスタマーフィードバック

Data from [Data independently produced by , , Protein Cell, 2017, 8(4):273-283]

Data from [Data independently produced by , , Wound Repair Regen, 2017, 25(3):526-531]

Data from [Data independently produced by , , Dev Biol, 2017,421(2):149-160]

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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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