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StemRegenin 1

Catalog No. T1831 CAS 1227633-49-9

Synonyms: SR1

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

StemRegenin 1, CAS 1227633-49-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 33.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 98.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 302.00
200 mg	In stock	$ 464.00
1 mL * 10 mM (in DMSO)	In stock	$ 36.00

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Purity: 99.78%

Purity: 99.66%

Purity: 99.06%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor.
Targets&IC50	AhR:127 nM
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.
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.
Kinase Assay	Kinase assays: PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.
Cell Research	StemRegenin 1 (SR1) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. 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].

Synonyms	SR1
Molecular Weight	429.54
Formula	C24H23N5OS
CAS No.	1227633-49-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (186.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Boitano AE, et al. Science, 2010, 329(5997), 1345-1348. 2. Gao H, et al. J Biol Chem, 2012, 287(35), 219979-291987. 3. Gori JL, et al. Blood, 2012, 120(13), e35-44. 4. Jin H, Ji C, Ren F, et al. AHR-Mediated Oxidative Stress Contributes to the Cardiac Developmental Toxicity of Trichloroethylene in Zebrafish Embryos[J]. Journal of Hazardous Materials. 2020, 385: 121521.

Citations

1. Jin H, Ji C, Ren F, et al. AHR-Mediated Oxidative Stress Contributes to the Cardiac Developmental Toxicity of Trichloroethylene in Zebrafish Embryos. Journal of Hazardous Materials. 2020, 385: 121521

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Transcription Factor-Targeted Compound Library Bioactive Compounds Library Max Bioactive Lipid Compound Library NO PAINS Compound Library Nuclear Receptor Compound Library Human Metabolite Library Target-Focused Phenotypic Screening Library Clinical Compound Library

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Keywords

StemRegenin 1 1227633-49-9 Immunology/Inflammation Metabolism Aryl Hydrocarbon Receptor AhR StemRegenin-1 SR1 StemRegenin1 inhibit Inhibitor SR-1 SR 1 inhibitor

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