RepSox (E-616452)

別名: SJN 2511,ALK5 Inhibitor II

目錄號：S7223 Purity: 99.97%

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II)是一種有效的，選擇性TGFβR-1/ALK5抑制劑，作用于ATP與ALK5結合以及ALK5自磷酸化，無細胞試驗中IC50分別為23 nM和4 nM。

RepSox (E-616452) Chemical Structure

CAS: 446859-33-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1303.16	現(xiàn)貨
10mg	1211.06	現(xiàn)貨
25mg	2219.57	現(xiàn)貨
100mg	5561.01	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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批次：純度： 99.97%

99.97

相關靶點	ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 TGFβRII TGF-β Smad3 Smad4 Smad5 ALK7	點擊展開
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細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息(PMID)
HeLa	Function assay	1 uM	30 mins	Inhibition of ALK5 in serum starved human HeLa cells assessed as reduction in TGF-beta-induced SMAD2/3 nuclear transaction at 1 uM pre-incubated for 30 mins before TGF-beta stimulation for 30 mins by immunofluorescence analysis	28135685
HepG2 cells	Function assay			Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells, IC50=10 nM	15317461
baculovirus/Sf9 cells	Function assay			Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells, IC50=4 nM	15317461
Sf9	Function assay			Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate in presence of [gamma-33P]ATP, IC50 = 0.181 μM.	28135685
Sf9	Function assay			Inhibition of mouse ABL expressed in Sf9 insect cells using GGEAIYAAPFKK as substrate in presence of [gamma-33P]ATP, IC50 = 21 μM.	28135685
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產品描述

靶點

TGFβR1(ALK5) ^[1]
(Cell-free assay)

4 nM


體外研究(In Vitro)
體外研究活性	RepSox抑制ATP結合到ALK5和抑制ALK5自磷酸化，IC50分別為23 nM和4 nM。RepSox抑制TGF-β 誘導的細胞PAI-1熒光素酶活性，IC50為18 nM。^[1] RepSox在重編程中通過抑制轉化生長因子-β(Tgf-β)信號，能夠成功取代Sox2，這反過來又導致Nanog表達。RepSox誘導重編程不需要染色質重塑。RepSox對產生iPSCs是有效的。^[2]
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot