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1227633-49-9

1227633-49-9 structure
1227633-49-9 structure
  • Name: StemRegenin 1 (SR1)
  • Chemical Name: 4-[2-[[2-(1-benzothiophen-3-yl)-9-propan-2-ylpurin-6-yl]amino]ethyl]phenol
  • CAS Number: 1227633-49-9
  • Molecular Formula: C24H23N5OS
  • Molecular Weight: 429.537
  • Catalog: Biochemical Inhibitor Metabolism AhR antagonist
  • Create Date: 2017-06-03 04:14:06
  • Modify Date: 2025-08-25 12:01:48
  • StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.

Name 4-[2-[[2-(1-benzothiophen-3-yl)-9-propan-2-ylpurin-6-yl]amino]ethyl]phenol
Synonyms 4-(2-{[2-(1-Benzothiophen-3-yl)-9-isopropyl-9H-purin-6-yl]amino}ethyl)phenol
Phenol, 4-[2-[[2-benzo[b]thien-3-yl-9-(1-methylethyl)-9H-purin-6-yl]amino]ethyl]-
StemRegenin1
StemRegenin 1
SR1
Description StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
Related Catalog
Target

IC50: 127 nM (AhR)[1]

In Vitro StemRegenin 1 (SR1) acts by antagonizing the aryl hydrocarbon receptor (AhR). StemRegenin 1 increases the number of CD34+ cells after 5 to 7 days with an EC50 of ~120 nM. StemRegenin 1 inhibits photoaffinity ligand (PAL) binding (IC50=40 nM) These results support the conclusion that StemRegenin 1 -induced CD34+ cell expansion is mediated through direct binding and inhibition of the AhR[1]. An aryl hydrocarbon receptor antagonist, StemRegenin 1 (SR1), robustly promotes ex vivo expansion of human CD34+ cells. StemRegenin 1 treatment accelerates the proliferation of CD34+ cells and decreases the expression levels of VentX[2].
Cell Assay A quantity of 250,000 CB-derived CD34+ cells are cultured with control conditions (DMSO, 0.01%) or StemRegenin 1 (0.75 μM) for 3 weeks. At this point control cultures had expanded 1080-fold and StemRegenin 1 treated cells expanded 2024-fold relative to starting cell numbers. A quantity of 30 to 30,000 uncultured CD34+ CB-derived cells or a fraction of the final culture equivalent to 30 to 10,000 starting cells are transplanted. The cells are injected intravenously via the retro-orbital route into sub-lethally irradiated (300 rads, 200 rads) 6- to 10-week-old NSG mice. Engraftment is performed within 24 h after irradiation. Engraftment is monitored by flow cytometric analysis of blood obtained via retro-orbital sinus or bone marrow using anti-human CD45 and anti-mouse CD45 antibodies. The mice are sacrificed between 13-16 weeks posttransplantation; bone marrow (from both femurs and tibiae), spleen and thymus are collected for analysis. For secondary engraftment, 50% of the bone marrow from each recipient mouse is transplanted into one secondary sub-lethally irradiated NSG mouse. Fifteen weeks after transplantation, bone marrow is harvested from the secondary mice and analyzed by flow cytometry[1].
References

[1]. Boitano AE, et al. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells. Science. 2010 Sep 10;329(5997):1345-8.

[2]. Gao H, et al. Suppression of homeobox transcription factor VentX promotes expansion of human hematopoietic stem/multipotent progenitor cells. J Biol Chem. 2012 Aug 24;287(35):29979-87.

Density 1.4±0.1 g/cm3
Boiling Point 622.9±65.0 °C at 760 mmHg
Molecular Formula C24H23N5OS
Molecular Weight 429.537
Flash Point 330.5±34.3 °C
Exact Mass 429.162323
PSA 104.10000
LogP 5.10
Appearance white solid
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.721
Storage condition +2C to +8C
Hazard Codes Xn
Risk Phrases 22
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