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Cat. No. Product Name CAS No. Information
PC-35521

WRG-28

1913291-02-7

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

PC-35847

DDR-TRK-1

1912357-12-0 DDR-TRK-1 (DDR1 inhibitor 6j) is a potent, selective selective DDR1 inhibitor with IC50 of 9.4 nM, also potently inhibits TRK family with IC50 of 18-100 nM; DDR-TRK-1 inhibits colony formation and migration of Panc-1 pancreatic cancer cells. In cellular and mouse models of lung fibrosis, DDR-TRK-1 inhibits signaling, expression of fibrotic markers and fibrotic features such as hydroxproline expression; DDR-TRK-1 is selective in KINOMEscan at 1 uM,t he closest off target is CDK11 (370 nM).
PC-35802

DDR1 inhibitor 2.45

2125676-13-1 DDR1 inhibitor 2.45 (Compound 2.45) is a novel potent, selective, bioavailable Discoidin Domain Receptor 1 (DDR1) inhibitor with IC50 of 29 nM, displays 64-fold selectivity over DDR2 in biochemical assays; also possesses excellent kinome selectivity against a kinase panel of 468 kinases; Compound 2.45 inhibits DDR1 phosphorylation (70% inhibition at 1 uM in HT1080 cells overexpressing DDR1) and recruitment of SHC1 in vitro, and modulates phenotype of collagen stimulated renal epithelial cells; Compound 2.45 preserves renal function and reduces tissue damage in Col4a3−/− mice (the preclinical mouse model of Alport syndrome).
PC-35543

Dual DDR1 and DDR2 inhibitor 5n

Dual DDR1 and DDR2 inhibitor 5n is a highly potent, selective, dual Discoidin domain receptor DDR1 and DDR2 inhibitor with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively; displays significant selectivity against a panel of 403 wild-type kinases at 1 uM (Abl1 IC50=494 nM); dose-dependently inhibited lipopolysaccharide (LPS)-induced interleukin-6 (IL-6) release in mouse primary peritoneal macrophages (MPMs), attenuates lung pathophysiologic changes in LPS-challenged mice, effectively decreases the levels of TNF-α and IL-6 both in BALF and serum.
PC-35349

DDR inhibitor X

1644069-80-6 DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
PC-63520

LCB 03-0110 dihydrochloride

1962928-28-4 LCB 03-0110 is a potent, ATP-competitive inhibitor of Discoidin domain receptor (DDR) family and c-Src tyrosine kinase family, as well as Btk and Syk; potently inhibits the activated tyrosine kinase activity of DDR2 (IC50=6 nM), and nonactivated form of DDR2 (IC50=145 nM); suppresses collagen-induced autophosphorylation of DDR1 and DDR2 with IC50 of 164 and 171 nM in cell-based assays; inhibits all eight Src family kinases with IC50 of 2-20 nM; suppresses the proliferation and migration of primary dermal fibroblasts induced by TGF β1 and type I collagen (IC50=194 nM), inhibits cell migration and nitric oxide, iNOS, COX2, and TNF-α synthesis in LPS-activated J774A.1 macrophage cells; suppresses hypertrophic scar formation in wound healing models.
PC-63519

LCB 03-0110

1228102-01-9 LCB 03-0110 is a potent, ATP-competitive inhibitor of Discoidin domain receptor (DDR) family and c-Src tyrosine kinase family, as well as Btk and Syk; potently inhibits the activated tyrosine kinase activity of DDR2 (IC50=6 nM), and nonactivated form of DDR2 (IC50=145 nM); suppresses collagen-induced autophosphorylation of DDR1 and DDR2 with IC50 of 164 and 171 nM in cell-based assays; inhibits all eight Src family kinases with IC50 of 2-20 nM; suppresses the proliferation and migration of primary dermal fibroblasts induced by TGF β1 and type I collagen (IC50=194 nM), inhibits cell migration and nitric oxide, iNOS, COX2, and TNF-α synthesis in LPS-activated J774A.1 macrophage cells; suppresses hypertrophic scar formation in wound healing models.

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