Chemical Structure : WR-S-462
CAS No.:
WR-S-462
Catalog No.: PC-25257Not For Human Use, Lab Use Only.
WR-S-462 is a highly potent and selective STAT3 inhibitor with SPR Kd of 58 nM, directly interferes with the STAT3-SH2 domain interaction.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
WR-S-462 is a highly potent and selective STAT3 inhibitor with SPR Kd of 58 nM, directly interferes with the STAT3-SH2 domain interaction.
WR-S-462 significantly disrupts STAT3 nuclear localization and inhibits STAT3 Y705 phosphorylation both in MDA-MB-231 and BT549 cells.
WR-S-462 exhibits little inhibitory effects on JAK1, JAK2, JAK3, EGFR, and SRC kinases, shows no discernible impact on the phosphorylation levels of JAK1, ERK1/2, AKT, STAT1, and STAT5.
WR-S-462 selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells.
WR-S-462 strongly suppresses the colony formation of TNBC cells.
WR-S-462 forcefully suppresses the migration and invasion of TNBC cells.
WR-S-462 promotes TNBC cell apoptosis, inhibits tumor growth in preclinical TNBC xenografts.
Physicochemical Properties
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M.Wt
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462.52
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Formula
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C24H22N4O4S
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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-Cyano-2-(3-methoxybenzamido)-N-(2-methoxyphenyl)-4,7-dihydrothieno[2,3-c] pyridine-6(5H)-carboxamide
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References
1. Jin W, et al. Eur J Med Chem. 2025 Apr 5;287:117332.
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