STAT3 inhibitor LY5

Chemical Structure : STAT3 inhibitor LY5

Catalog No.: PC-20632Not For Human Use, Lab Use Only.

STAT3 inhibitor LY5 is a specfic STAT3 small molecule inhibitor, binds to STAT3 SH2 domain wioth Kd of 2.5 uM.

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Biological Activity

STAT3 inhibitor LY5 is a specfic STAT3 small molecule inhibitor, binds to STAT3 SH2 domain wioth Kd of 2.5 uM.
LY5 (0.5-1 uM, 8 h) inhibits constitutive STAT3 phosphorylation in Ewing's sarcoma cell line EW8.
LY5 (0.25-1 uM) inhibits IL-6 induced STAT3 phosphorylation in MCF-7 cells, but not STAT1 phosphorylation induced by IFN-γ.
LY5 induces apoptosis in human sarcoma cells (RD2, RH30,and U2OS) with IC50 of 0.5-1.4 uM.
LY5 (5 mg/kg, IP) suppresses tumor growth of MDA-MB-231 breast cancer cells in mouse tumor model in vivo.
LY5 down-regulates the expression of the downstream targets of STAT3, including cyclin D1, bcl-XL, survivin, and micro-RNA-21, in human medulloblastoma cells.
LY5 inhibits the induction of STAT3 phosphorylation by IL-6, IGF-1, IGF-2, and leukemia inhibitory factor in medulloblastoma cells, but does not inhibit STAT1 and STAT5 phosphorylation stimulated by IFN-γ and EGF, respectively.
LY5 blocks the STAT3 nuclear localization induced by IL-6, but does not block STAT1 and STAT5 nuclear translocation mediated by IFN-γ and EGF, respectively.

Physicochemical Properties

M.Wt	329.33
Formula	C15H11N3O4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=S(C(C=CC=C1C(C(NC2=CC=CN=C2)=C3)=O)=C1C3=O)(N)=O

References

1. Yu W, et al. J Med Chem. 2013 Jun 13;56(11):4402-12.

2. Xiao H, et al. J Biol Chem. 2015 Feb 6;290(6):3418-29.

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