StemRegenin 1

SKU: orb1307360

Description

StemRegenin 1 (SR1) is a potent and selective small molecule antagonist of the aryl hydrocarbon receptor (AhR). It is widely used in research to expand hematopoietic stem cells in vitro and has been applied in studies investigating hematopoiesis, immune regulation, and toxicology.

Research Area

Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 1227633-49-9
• MW: 429.54
• Purity: ≥98% (May vary between batches)
• Formula: C₂₄H₂₃N₅OS
• SMILES: CC(C)n1cnc2c(NCCc3ccc(O)cc3)nc(nc12)-c1csc2ccccc12
• Target: AhR,Aryl Hydrocarbon Receptor
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.66 mM);DMSO:123.75 mg/mL (288.1 mM)

Bioactivity

• Target IC50:
  AhR:127 nM
• In Vivo:
  In vitro, StemRegenin 1 (1 μM) effectively promotes the proliferation of CD34+ cells (EC50 ≈ 120 nM) while concurrently reducing the expression levels of VentX. Furthermore, StemRegenin 1 can inhibit the binding of photoaffinity ligands (PAL) with an IC50 value of 40 nM.
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• In Vitro:
  In NSG (NOD.Cg-Prkdcscid Il2rgtm1Wj1/SzJ) mice, the proliferation of CB CD34+ cells is enhanced through the activation of SR1, facilitating early and sustained cell engraftment.
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• Cell Research:
  StemRegenin 1 (SR1) is prepared in DMSO and stored, and then diluted with appropriate medium before use. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ArylHydrocarbonReceptor, Aryl Hydrocarbon Receptor, AhR, inhibit, Inhibitor, StemRegenin 1, StemRegenin1, StemRegenin-1, SR 1, SR1, SR-1

Compound Identifiers

PubChem CID

46199207