StemRegenin 1 (SR1)

Catalog No.S2858

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

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StemRegenin 1 (SR1) Chemical Structure

StemRegenin 1 (SR1) Chemical Structure
Molecular Weight: 429.54

Validation & Quality Control

Quality Control & MSDS

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StemRegenin 1 (SR1) is available in the following compound libraries:

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Product Description

Biological Activity

Description 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]
IC50 127 nM
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]
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]

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Boitano AE, et al. Science, 2010, 329(5997), 1345-1348.

[2] Gao H, et al. J Biol Chem, 2012, 287(35), 29979-29987.

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Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02827513 Terminated Adult Attention-deficit Hyperactivity Disorder (ADHD) Neurovance, Inc.|Euthymics BioScience, Inc. December 2015 Phase 1
NCT01744808 Completed Normal, Healthy Volunteers Neurovance, Inc.|Euthymics BioScience, Inc. February 2013 Phase 1
NCT00557973 Completed Muscle Spasticity Indivior Inc. December 2007 Phase 2

Chemical Information

Download StemRegenin 1 (SR1) SDF
Molecular Weight (MW) 429.54


CAS No. 1227633-49-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 86 mg/mL (200.21 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Phenol, 4-[2-[[2-benzo[b]thien-3-yl-9-(1-methylethyl)-9H-purin-6-yl]amino]ethyl]-

Tech Support

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