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YY002

Chemical Structure : YY002

CAS No.: 2591440-75-2

YY002 (YY-002)

Catalog No.: PC-22095Not For Human Use, Lab Use Only.

YY002 is a potent, selective STAT3 inhibitor, selectively binds to the STAT3 Src Homology 2 (SH2) domain (KD=2.24 nM) over other STAT members, inhibits STAT3 Tyr705 and Ser727 phosphorylation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

YY002 is a potent, selective STAT3 inhibitor, selectively binds to the STAT3 Src Homology 2 (SH2) domain (KD=2.24 nM) over other STAT members, inhibits STAT3 Tyr705 and Ser727 phosphorylation.
YY002 strongly suppresses STAT3 nuclear and mitochondrial functions in STAT3-dependent cells.
YY002 also shows no obvious inhibition on tyrosine kinases or serine kinases.
YY002 potently suppresses pancreatic cancer cells with high pSTAT3 (Tyr705 and Ser727) with IC50 of 3-11 nM.
YY002 inhibitscolony formation of multiple STAT3-dependent PDAC cells at concentration of 1 to 10 nM.
YY002 inhibits STAT3 Ser727 phosphorylation and mitochondrial OXPHOS.
YY002 (5 mg/kg/d to 20 mg/kg/d, oral) inhibits pancreatic cancer growth in PANC-1 tumor mouse xenograft models.

Physicochemical Properties

M.Wt 737.66
Formula C36H29F6N7O4
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

(1-methyl-6-((5-(3-(4-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-5-yl)pyrazin-2-yl)oxy)-1H-indol-2-yl)(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazin-1-yl)methanone

References

1. Huang Chen, et al. ACS Cent Sci. 2024 Feb 10;10(3):579-594.

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