Stemregenin 1
Based on 17 publication(s) in Google Scholar
Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 1227633-49-9
- Formula: C24H23N5OS
- Molecular Weight:429.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Stemregenin 1
More- Cell. 2025 Oct 16;188(21):5878-5894.e18. [Abstract]
- Cell Stem Cell. 2024 Jun 6;31(6):803-817.e6. [Abstract]
- Nat Commun. 2024 Jun 8;15(1):4909. [Abstract]
- Theranostics. 2021 Aug 11;11(18):8797-8812. [Abstract]
- J Adv Res. 2026 Feb 11:S2090-1232(26)00141-4. [Abstract]
- Sci Adv. 2022 Mar 18;8(11):eabf8627. [Abstract]
- J Hazard Mater. 2020 Mar 5;385:121521. [Abstract]
- Int J Biol Macromol. 2023 Dec 31;253(Pt 3):126920. [Abstract]
- Stem Cell Res Ther. 2025 May 1;16(1):216. [Abstract]
- Cell Chem Biol. 2026 Jan 15;33(1):91-101.e12. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 1:269:115782. [Abstract]
- Biochem Pharmacol. 2023 Dec:218:115934. [Abstract]
- Food Funct. 2021 Apr 7;12(7):3191-3205. [Abstract]
- RSC Adv. 2022 Apr 13;12(18):11505-11516. [Abstract]
- bioRxiv. 2026 Mar 29:2026.03.27.714536. [Abstract]
- SSRN. 2025 Jul 25.
- Patent. US20180263995A1.
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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RT-PCR
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WB
Biological Activity
IC50: 127 nM (AhR)[1]
Stemregenin 1 (SR1) acts by antagonizing the aryl hydrocarbon receptor (AhR). Stemregenin 1 increases the number of CD34+ cells after 5 to 7 days with an EC50 of ~120 nM. Stemregenin 1 inhibits photoaffinity ligand (PAL) binding (IC50=40 nM) These results support the conclusion that Stemregenin 1 -induced CD34+ cell expansion is mediated through direct binding and inhibition of the AhR[1]. An aryl hydrocarbon receptor antagonist, Stemregenin 1 (SR1), robustly promotes ex vivo expansion of human CD34+ cells. Stemregenin 1 treatment accelerates the proliferation of CD34+ cells and decreases the expression levels of VentX[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1227633-49-9
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Appearance Solid
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Molecular Weight 429.54
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Formula C24H23N5OS
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Color White to off-white
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SMILES
CC(C)N1C2=NC(C3=CSC4=C3C=CC=C4)=NC(NCCC5=CC=C(O)C=C5)=C2N=C1
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Synonyms
SR1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Cell
Composite transposons with bivalent histone marks function as RNA-dependent enhancers in cell fate regulation. [Abstract]2025 Oct 16;188(21):5878-5894.e18. PMID: 40774253 -
Cell Stem Cell
Human anti-PSCA CAR macrophages possess potent antitumor activity against pancreatic cancer. [Abstract]2024 Jun 6;31(6):803-817.e6. PMID: 38663406 -
Nat Commun
Tobacco-induced hyperglycemia promotes lung cancer progression via cancer cell-macrophage interaction through paracrine IGF2/IR/NPM1-driven PD-L1 expression. [Abstract]2024 Jun 8;15(1):4909. PMID: 38851766
Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 8;15(1):4909. [Abstract]
Stemregenin 1 (S: SR1; 1 μM; 3 days). WB of GLUT1 and GLUT3 expression in WCL and MEM fraction.
Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 8;15(1):4909. [Abstract]
Stemregenin 1 (S: SR1; 1 μM; 3 days). Operetta high content imaging analysis of 2-NBDG fluorescent tracer uptake.
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Theranostics
Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin. [Abstract]2021 Aug 11;11(18):8797-8812. PMID: 34522212
Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Aug 11;11(18):8797-8812. [Abstract]
N2a cells were treated with Dio (80 μM) with or without SR1 (2 μM) for 12 h. Whole cell lysates were collected and the NEP levels were determined.
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J Adv Res
2026 Feb 11:S2090-1232(26)00141-4. PMID: 41687771 -
Sci Adv
2022 Mar 18;8(11):eabf8627. PMID: 35302840 -
J Hazard Mater
AHR-mediated oxidative stress contributes to the cardiac developmental toxicity of trichloroethylene in zebrafish embryos. [Abstract]2020 Mar 5;385:121521. PMID: 31699484 -
Int J Biol Macromol
Therapeutic mechanism exploration of polysaccharides from Dendrobium officinale on unilateral ureteral obstruction operation-induced renal fibrosis based on improving oxidative stress injury mediated by AhR/NOX4 pathway. [Abstract]2023 Dec 31;253(Pt 3):126920. PMID: 37717864 -
Stem Cell Res Ther
DSUP modified mesenchymal stem cells exert significant radiation protective effect by enhancing the hematopoietic niche. [Abstract]2025 May 1;16(1):216. PMID: 40312405 -
Cell Chem Biol
Identification of aryl hydrocarbon receptor as a functional target that enhances astrocytic ApoE secretion. [Abstract]2026 Jan 15;33(1):91-101.e12. PMID: 41483807 -
Ecotoxicol Environ Saf
2024 Jan 1:269:115782. PMID: 38056121 -
Biochem Pharmacol
Hydroquinone-selected chronic myelogenous leukemia cells are sensitive to chloroquine-induced cytotoxicity via MCL1 suppression and glycolysis inhibition. [Abstract]2023 Dec:218:115934. PMID: 37989415 -
Food Funct
Fructooligosaccharides protect against OVA-induced food allergy in mice by regulating the Th17/Treg cell balance using tryptophan metabolites. [Abstract]2021 Apr 7;12(7):3191-3205. PMID: 33735338 -
RSC Adv
Beneficial roles of the AhR ligand FICZ on the regenerative potentials of BMSCs and primed cartilage templates. [Abstract]2022 Apr 13;12(18):11505-11516. PMID: 35425032
Stemregenin 1 purchased from MedChemExpress. Usage Cited in: RSC Adv. 2022 Apr 13;12(18):11505-11516. [Abstract]
Stemregenin 1 (SR1; 1 μM; 0-5 days).The absorbance at 450 nm of the CCK8 assay of the BMSCs. The number of viable BMSCs increased in all groups and there were no significant differences among the three groups on days 0, 1, 3 and 5 (p < 0.05).
Stemregenin 1 purchased from MedChemExpress. Usage Cited in: RSC Adv. 2022 Apr 13;12(18):11505-11516. [Abstract]
Stemregenin 1 (SR1; 1 μM; 0-5 days).RT-PCR demonstrated that FICZ or SR1 prevented or exacerbated LPS-induced IL-1β, 6 and TNF-α, respectively.
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bioRxiv
Epigenome editing of human hematopoietic stem cells enables sustained and reversible thrombosis prevention. [Abstract]2026 Mar 29:2026.03.27.714536. PMID: 41928991 -
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Solvent & Solubility
DMSO : 62.5 mg/mL (145.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Boitano AE, et al. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells. Science. 2010 Sep 10;329(5997):1345-8. [Content Brief]
[2]. Gao H, et al. Suppression of homeobox transcription factor VentX promotes expansion of human hematopoietic stem/multipotent progenitor cells. J Biol Chem. 2012 Aug 24;287(35):29979-87. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3281 mL | 11.6404 mL | 23.2807 mL | 58.2018 mL |
| 5 mM | 0.4656 mL | 2.3281 mL | 4.6561 mL | 11.6404 mL | |
| 10 mM | 0.2328 mL | 1.1640 mL | 2.3281 mL | 5.8202 mL | |
| 15 mM | 0.1552 mL | 0.7760 mL | 1.5520 mL | 3.8801 mL | |
| 20 mM | 0.1164 mL | 0.5820 mL | 1.1640 mL | 2.9101 mL | |
| 25 mM | 0.0931 mL | 0.4656 mL | 0.9312 mL | 2.3281 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7760 mL | 1.9401 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5820 mL | 1.4550 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1640 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9700 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7275 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5820 mL |