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RepSox

现货
Catalog No.
A3754
ALK5抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 900.00
现货
25mg
¥ 1,650.00
现货

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Background

RepSox is a potent and selective inhibitor of the TGFβR-1 with IC50 of 23 nM [1].

TGFβR-1 belongs to the TGFβ receptor family, which is a serine/threonine kinase receptor and bind ligand TGFβ. It gets involved in tumor transformation, cell differentiation and proliferation.

RepSox was found to replace the function of Sox2 to induce reprogramming of iPS cells, via the mechanism of inhibiting TGFβR-1 [1]. MEF cells were treated with RepSox for 3 days, and then it was removed at the time of transduction with Oct4, Klf4, and cMyc. The result showed the TGFβR-1 -associated expression of L-Myc was increased by 5-fold after RepSox treatment [1]. A partially reprogrammed cell line (OKMS 6) was treated with RepSox and performed global gene expression analysis at 10, 24, and 48 hours following the initiation of treatment. The result showed the Id1, Id2 and Id3 gene, repressed by TGFβR-1 signaling, were released from that repression and the expression level was increased. Additionally, other genes responsive for TGFβR-1 signaling were inhibited. It suggested RepSox was able to inhibit TGFβR-1 and suppress the TGFβR-1 downstream signaling [1].

In mouse model, iPS cells reprogrammed by RepSox were labeled with Tomato-red protein and then they were injected mouse blastocysts to produce mosaic embryo. The result showed that both embryo and adult mouse were with significant contribution from RepSox induced iPS cells. It suggested that the inhibitory activity of RepSox for TGFβR-1 was active in vivo [1].

Reference:
[1] Ichida J K et al. , A small molecule inhibitor of Tgaf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell, 2009, 5(5): 491-503.

Chemical Properties

StorageStore at -20°C
M.Wt287.32
Cas No.446859-33-2
FormulaC17H13N5
SynonymsE-616452;SJN 2511;E616452;SJN2511;E 616452;SJN-2511,ALK5 Inhibitor II
Solubility≥14.35 mg/mL in DMSO, ≥47.9 mg/mL in EtOH with gentle warming, <2.22 mg/mL in H2O
Chemical Name2-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]-1,5-naphthyridine
SDFDownload SDF
Canonical SMILESCC1=CC=CC(=N1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

MEFs

制备方法

在DMSO中的溶解度大于14.4 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

25 μ M;3天

实验结果

使用RepSox对MEF进行预处理,再对其进行Oct4, Klf4和cMyc转染,没有形成Oct4::GFP+集落。结果表明,经过RepSox处理后,TGFβR-1相关的L-Myc表达增加了5倍。

References:

[1]. Ichida J K et al. , A small molecule inhibitor of Tgaf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell, 2009, 5(5): 491-503.

生物活性

Description RepSox是TGFβ I型受体ALK5的选择性抑制剂,IC50值为4 nM。
靶点 ALK5          
IC50 4 nM          

质量控制

化学结构

RepSox