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WRG-28

Chemical Structure : WRG-28

CAS No.: 1913291-02-7

WRG-28 (DDR2 inhibitor WRG-28;WRG28)

Catalog No.: PC-35521Not For Human Use, Lab Use Only.

WRG-28 (DDR2 inhibitor WRG-28) is a potent, selective, allosteric inhibitor of discoidin domain receptor 2 (DDR2) with binding IC50 of 230 nM.

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Biological Activity

WRG-28 (DDR2 inhibitor WRG-28) is a potent, selective, allosteric inhibitor of discoidin domain receptor 2 (DDR2) with binding IC50 of 230 nM.
WRG-28 bluntsd collagen I-mediated DDR2 tyrosine phosphorylation, ERK activation, and SNAIL1 protein stabilization (IC50=286 nM) in HEK293 cells expressing DDR2, without effect on normal mammary epithelial MCF10A cells.
WRG-28 displays no activity against collagen I-induced tyrosine phosphorylation of the related DDR1 RTK in HEK293 cells.
WRG-28 inhibits DDR2-collagen interaction in an allosteric manner, inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs.

Physicochemical Properties

M.Wt 410.444
Formula C21H18N2O5S
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

N-ethyl-4-(((3-oxo-3H-phenoxazin-7-yl)oxy)methyl)benzenesulfonamide

References

1. Grither WR, et al. Proc Natl Acad Sci U S A. 2018 Jul 30. pii: 201805020.

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