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StemRegenin 1 (hydrochloride)

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aryl hydrocarbon receptor signaling antagonist
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IC50: 127 nM in CD34+ cells

StemRegenin 1 is an aryl hydrocarbon receptor signaling antagonist.

The aryl hydrocarbon receptor (AhR ) is a protein that is encoded by the AHR gene. The AhR is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons.

In vitro: In previous study, the unbiased screen with primary human HSCs identified the StemRegenin 1 (SR1), which could promote the ex-vivo expansion of CD34+ cells. In addition, the culture of HSCs with SR1 resulted in a 50-fold increase in cells expressing CD34. Moreover, the mechanistic studies showed that SR1 acted by antagonizing the AhR [1].

In vivo: In aninmal study, 300 to 30,000 uncultured CB CD34+ cells were transplanted into NSG mice. Results showed that CB CD34+ cells cultured with SR1 led to significant increases in human engraftment in the peripheral blood at 1 week, compared with mice transplanted with 10,000 uncultured cells or the progeny of 10,000 control cells [1].

Clinical trial: An open label, randomized phase II trial comparing SR-1 cultured umbilical cord blood to unmanipulated umbilical cord blood transplantation after a myeloablative CY/FLU/TBI conditioning has been proposed, but is not yet open for participant recruitment [2].

[1] A.  E. Boitano, J. Wang, R. Romeo, et al. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science 329,1345-1348 (2010).
[2] https://clinicaltrials. gov/ct2/show/NCT02765997 term=StemRegenin+1&rank=1

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
FormulaC24H23N5OS • HCl
Solubility≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name4-(2-((2-(benzo[b]thiophen-3-yl)-9-isopropyl-9H-purin-6-yl)amino)ethyl)phenol, monohydrochloride
SDFDownload SDF
Canonical SMILESOC1=CC=C(C=C1)CCNC2=C3C(N(C(C)C)C=N3)=NC(C4=CSC5=C4C=CC=C5)=N2.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

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Chemical structure

StemRegenin 1 (hydrochloride)