For research use only. Not for therapeutic Use.
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice[1][2].
WRG-28 (1, 2 μM; 4 h) blunts collagen I-mediated DDR2 tyrosine phosphorylation and (1 μM; 7 h) ERK activation as well as SNAIL1 protein stabilization in HEK293 cells (expressing DDR2) (IC50=286 nM)[1].
WRG-28 (1 μM; 48 h) blunts tumor cell invasion and migration by inhibiting DDR2 in BT549 and 4T1 breast cancer cells[1].
WRG-28 (1 μM; 4 days) inhibits tumor-promoting effects of CAFs[1].
WRG-28 (0.5, 1 μM; 4 h) maintains inhibitory action toward acquired DDR2 mutations that are resistant to TKIs[1].
WRG-28 (10 mg/kg; i.v.; single) attenuates biochemical signaling of DDR2 in breast tumors in vivo[1].
WRG-28 (10 mg/kg; i.v.; single daily for 7 days) reduces metastatic lung colonization of breast tumor cells[1].
WRG-28 (10 mg/kg; i.v.; single daily for 21 days) decreases both the inflammatory reaction and joint destruction in mice with collagen antibody-induced arthritis (CAIA)[2].
| Catalog Number | I018175 |
| CAS Number | 1913291-02-7 |
| Synonyms | N-ethyl-4-[(7-oxophenoxazin-3-yl)oxymethyl]benzenesulfonamide |
| Molecular Formula | C21H18N2O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H18N2O5S/c1-2-22-29(25,26)17-7-3-14(4-8-17)13-27-16-6-10-19-21(12-16)28-20-11-15(24)5-9-18(20)23-19/h3-12,22H,2,13H2,1H3 |
| InChIKey | AARVTLIQNGAELZ-UHFFFAOYSA-N |
| SMILES | CCNS(=O)(=O)C1=CC=C(C=C1)COC2=CC3=C(C=C2)N=C4C=CC(=O)C=C4O3 |
| Reference | [1]. Grither WR, et al. Inhibition of tumor-microenvironment interaction and tumor invasion by small-molecule allosteric inhibitor of DDR2 extracellular domain. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7786-E7794. [2]. Mu N, et al. Blockade of Discoidin Domain Receptor 2 as a Strategy for Reducing Inflammation and Joint Destruction in Rheumatoid Arthritis Via Altered Interleukin-15 and Dkk-1 Signaling in Fibroblast-Like Synoviocytes. Arthritis Rheumatol. 2020 Jun;72(6):943-956. |
