受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H23N5OS |
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分子量 | 429.54 | CAS No. | 1227633-49-9 | |
Solubility (25°C)* | 体外 | DMSO | 86 mg/mL (200.21 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay. |
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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] |
キナーゼアッセイ | AhR ligand binding assay | |
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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. | ||
細胞アッセイ | 細胞株 | Cell-free assays |
濃度 | 127 nM | |
反応時間 | ||
実験の流れ |
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Data from [Data independently produced by , , Stem Cells Transl Med, 2017, 6(3):897-909]
TDO2 promotes bladder cancer progression via AhR-mediated SPARC/FILIP1L signaling [ Biochem Pharmacol, 2024, 223:116172] | PubMed: 38552852 |
ARID5A stabilizes Indoleamine 2,3-dioxygenase expression and enhances CAR T cell exhaustion in colorectal cancer [ Transl Oncol, 2024, 42:101900] | PubMed: 38316094 |
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] | PubMed: 38451784 |
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 |
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909] | PubMed: none |
Mapping human haematopoietic stem cells from haemogenic endothelium to birth [ Nature, 2022, 604(7906):534-540] | PubMed: 35418685 |
Adipocyte-derived kynurenine promotes obesity and insulin resistance by activating the AhR/STAT3/IL-6 signaling [ Nat Commun, 2022, 13(1):3489] | PubMed: 35715443 |
Relieving DYRK1A repression of MKL1 confers an adult-like phenotype to human infantile megakaryocytes [ J Clin Invest, 2022, 132-19e154839] | PubMed: 35925681 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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