SR1 (StemRegenin 1)

Catalog No.S2858 Batch:S285807

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Technical Data

Formula

C24H23N5OS
Molecular Weight 429.54 CAS No. 1227633-49-9
Solubility (25°C)* In vitro DMSO 86 mg/mL (200.21 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from 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.

Customer Product Validation

Data from [Data independently produced by , , Stem Cells Transl Med, 2017, 6(3):897-909]

Selleck's SR1 (StemRegenin 1) has been cited by 45 publications

Long-term engrafting multilineage hematopoietic cells differentiated from human induced pluripotent stem cells [ Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7] PubMed: 39223325
TDO2 promotes bladder cancer progression via AhR-mediated SPARC/FILIP1L signaling [ Biochem Pharmacol, 2024, 223:116172] PubMed: 38552852
StemRegenin 1 attenuates the RANKL-induced osteoclastogenesis via inhibiting AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway [ iScience, 2024, 27(5):109682] PubMed: 38660403
ARID5A stabilizes Indoleamine 2,3-dioxygenase expression and enhances CAR T cell exhaustion in colorectal cancer [ Transl Oncol, 2024, 42:101900] PubMed: 38316094
AHR signaling pathway mediates mitochondrial oxidative phosphorylation which leads to cytarabine resistance [ Acta Biochim Biophys Sin (Shanghai), 2024, 56(4):597-606] PubMed: 38404179
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] PubMed: 38451784
Aryl hydrocarbon receptor restricts axon regeneration of DRG neurons in response to injury [ bioRxiv, 2024, 2023.11.04.565649] PubMed: 37961567
Gut microbiota-derived 3-phenylpropionic acid promotes intestinal epithelial barrier function via AhR signaling [ Microbiome, 2023, 10.1186/s40168-023-01551-9] PubMed: 37158970
Gut microbiota-derived 3-phenylpropionic acid promotes intestinal epithelial barrier function via AhR signaling [ Microbiome, 2023, 11(1):102] PubMed: 37158970
Glutaminase inhibition in combination with azacytidine in myelodysplastic syndromes: Clinical efficacy and correlative analyses [ Res Sq, 2023, rs.3.rs-2518774] PubMed: 36865338

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.