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StemRegenin 1 (SR1)

现货
Catalog No.
A8224
AhR拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 500.00
现货
50mg
¥ 1,900.00
现货
100mg
¥ 3,300.00
现货
200mg
¥ 4,620.00
现货

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Background

StemRegenin 1 (SR1), a purine derivative, is a potent small molecule inhibitor of aryl hydrocarbon receptor (AhR) that potently antagonizes AhR with a value of 50% inhibition concentration IC50 of 127 nM in CD34+ cells. SR1 has been found to promote the ex vivo expansion of CD34+ cells. Recent study results have suggested that culture of hematopoietic stem cells (HSC) with SR1 increases cells expressing CD34 by fifty-fold and increases cells retaining the ability to engraft immunodeficient mice by 17-fold. SR1 has also been found to induce the ex vivo differentiation of pDCs, BDCA1+ and BDCA3+ mDCs as well as the generation of high numbers of all these DC subsets.

Reference

Thordardottir S, Hangalapura BN, Hutten T, Cossu M, Spanholtz J, Schaap N, Radstake TR, Vandervoort R, Dolstra H. The aryl hydrocarbon receptor antagonist StemRegenin 1 promotes human plasmacytoid and myeloid dendritic cell development from CD34+ hematopoietic progenitor cells. Stem Cells Dev. 2013 Dec 10. [Epub ahead of print]

Boitano AE, Wang J, Romeo R, Bouchez LC, Parker AE, Sutton SE, Walker JR, Flaveny CA, Perdew GH, Denison MS, Schultz PG, Cooke MP. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science. 2010 Sep 10;329(5997):1345-8. doi: 10.1126/science.1191536. Epub 2010 Aug 5.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt429.54
Cas No.1227633-49-9
FormulaC24H23N5OS
Solubility≥21.5mg/mL in DMSO, ≥3.41 mg/mL in EtOH with ultrasonic, <2.17 mg/mL in H2O
Chemical Name4-[2-[[2-(1-benzothiophen-3-yl)-9-propan-2-ylpurin-6-yl]amino]ethyl]phenol
SDFDownload SDF
Canonical SMILESCC(C)N1C=NC2=C1N=C(N=C2NCCC3=CC=C(C=C3)O)C4=CSC5=CC=CC=C54
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

CD34+UCB细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃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℃可放置数月。

反应条件

1 μM,3周

实验结果

用1 μM SR1或0.01% DMSO(对照)培养CD34+ UCB细胞,持续3周。在第7、14和21天测定总细胞数,并通过流式细胞术在每个时间点评价pDC的频率。在3周的培养期间,总成核细胞不断增加。时间点的pDC分化分析表明,在第14天达到pDCs的最大频率。在第21天,pDCs的绝对数目最高。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Thordardottir S, Hangalapura B N, Hutten T, et al. The Aryl Hydrocarbon Receptor Antagonist StemRegenin 1 Promotes Human Plasmacytoid and Myeloid Dendritic Cell Development from CD34+ Hematopoietic Progenitor Cells. Stem cells and development, 2013, 23(9): 955-967.

生物活性

描述 StemRegenin 1是AhR的抑制剂,IC50值为127 nM。
靶点 AhR          
IC50 127 nM          

质量控制

化学结构

StemRegenin 1 (SR1)

相关生物数据

StemRegenin 1 (SR1)

相关生物数据

StemRegenin 1 (SR1)