Chemical Structure : ST2 inhibitor XY52
CAS No.:
ST2 inhibitor XY52
Catalog No.: PC-21150Not For Human Use, Lab Use Only.
ST2 inhibitor XY52 is a specific small molecule inhibitor of soluble suppression of tumorigenesis-2 factor (ST2) with IC5 of 5.68 and 4.59 uM in ST2/IL-33 AlphaLISA and HEK-Blue reporter assays, repsectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ST2 inhibitor XY52 is a specific small molecule inhibitor of soluble suppression of tumorigenesis-2 factor (ST2) with IC5 of 5.68 and 4.59 uM in ST2/IL-33 AlphaLISA and HEK-Blue reporter assays, repsectively.
ST2 inhibitor XY52 shows 11-fold selectivity over ST2/IL1RAcP(IC50=64.3 uM) in AlphaLISA assay, inhibits more effectively the binding of IL-33 with sST2 than membrane ST2 bound with IL1RAcP.
ST2 inhibitor XY52 shows improved inhibitory activity and metabolic stability in vitro and in vivo than iST2-1 (Cat# PC-35645).
ST2 inhibitor XY52 (5-10 uM) induces dose-dependent reduction in CD4+ and CD8+ T-cell proliferation, with no significant toxicity to human peripheral blood mononuclear cells (PBMCs).
ST2 inhibitor XY52 (40 mg/kg BID, i.p. 21 days) reduces plasma sST2 and IFN-γ levels and GVHD score and extends survival in mice graft versus host disease (GVHD) model.
Physicochemical Properties
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M.Wt
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499.66
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Formula
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C30H37N5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(3-(1-((1-Ethyl-5-(2-methyl-4-nitrophenyl)-1H-pyrrol-2-yl)methyl)pyrrolidin-2-yl)phenyl)-3,8-diazabicyclo[3.2.1]octane
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References
1. Xinrui Yuan , et al. ACS Pharmacol Transl Sci. 2023 Aug 16;6(9):1275-1287.
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