Home Metabolism AhR antagonist SR1 (StemRegenin 1) For research use only.

SR1 (StemRegenin 1)

SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

SR1 (StemRegenin 1) Chemical Structure

SR1 (StemRegenin 1) Chemical Structure

CAS No. 1227633-49-9

Purity & Quality Control

SR1 (StemRegenin 1) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CD34+ Function assay Ex vivo expansion of human CD34+ cells assessed as increase in CD34+ cell level after 5 to 7 days by confocal microscopy, EC50=0.12μM 31035239
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Targets
Aryl hydrocarbon receptor (AhR) [1]
(Cell-free assay)
127 nM
In vitro
In vitro

StemRegenin 1 increases the number of CD34+ cells after 5 to 7 days with an EC50 of 120 nM. Culture of mPB CD34+ cells with cytokines plus SR1 (1 μM) for 7 days increases the number of CD34+, CD133+, and CD90+ hematopoietic stem and progenitor cell populations 2.6-, 2.3-, and 10-fold, respectively compared to control cells. Continued culture with SR1 (1 μM) for 3 weeks leads to an 11-fold increase in total nucleated cells (TNC), a 73-fold increase in CD34+ cells as compared to control cultures, and a 1118-fold increase in CD34+ cells relative to input cells. Culture of 1×103 cord blood CD34+ cells for 5 weeks with SR1 (1 μM) results in the production of 1.69×106 colony forming cells. SR1-induces CD34+ cell expansion acts by binding and antagonizing AhR as evident by decreased CYP1B1 and AHRR mRNA levels. [1]

SR1 (1 μM) treatment accelerates the proliferation of CD34+ cells and decreased the expression levels of VentX in human CD34+ cells. Ectopic expression of VentX prevents SR1-induced expansion of CD34+ cells. [2]

Sequential coculture with bone morphogenetic protein 4 (20 ng/mL), PGE2 (2 μM), and SR1 (0.75 μM) lead to robust Macaca nemestrina iPSC hematopoietic progenitor cell formation. CD34(+)CD38(-)Thy1(+)CD45RA(-)CD49f(+) cells isolated on the basis of CD34 expression and cultured in SR1 (0.75 μM) expands 3-fold and maintained this long-term repopulating HSC phenotype. [3]
Kinase Assay AhR ligand binding assay
Mouse livers are homogenized in buffer (25 mM MOPS, 2 mM EDTA, 0.02% NaN3, and 10% glycerol, pH 7.4) containing 20 mM sodium molybdate and protease inhibitors and centrifuged at 100,000g for 1 h. ligand-treated lysates are incubated at room temperature for 20 min and then photolyzes at 8 cm with 402 nm UV light. Dextran-coated charcoal (1%) is added to the photolyzed samples, which are then centrifuged at 3000g for 10 min to remove free ligand. Labeled samples are resolved using 8% acrylamide-tricine-SDS-PAGE, transferred to PVDF membrane, and visualized using autoradiography. Labeled AHR bands are excised and counted using a γ counter.
In Vivo
In vivo

SR1 promotes expansion of CB CD34+ cells that contribute to both early and sustained engraftment NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00763555 Completed
Psoriasis
Galderma R&D
 September 2008 Phase 2

Chemical Information & Solubility

Molecular Weight 429.54 Formula

C24H23N5OS
CAS No. 1227633-49-9 SDF Download SR1 (StemRegenin 1) SDF
Smiles CC(C)N1C=NC2=C(N=C(N=C21)C3=CSC4=CC=CC=C43)NCCC5=CC=C(C=C5)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (200.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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