MedChemExpress LLC (MCE)

MedChemExpress - Model WRG-28 - 1913291-02-7

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

MCE China：WRG-28

Brand：MedChemExpress (MCE)

Cat. No.HY-114169

CAS：1913291-02-7

Purity：99.34%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

In Vivo：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].

IC50 & Target：DDR2 230 nM (IC50)

References：

[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. [Content Brief]

[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. [Content Brief]

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