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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-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.
PC-63518

DDR1 inhibitor 7rh

1429617-90-2 DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays; DDR1 inhibitor 7rh is significantly less potent in suppressing the kinase activities of DDR2 (IC50=101 nM), Bcr-Abl (IC50=355 nM), and c-Kit (IC50>10 uM); inhibits DDR1-mediated signaling induced by soluble collagen (50 μg/ml) in a concentration-dependent manner, inhibits activation of PYK2 and PEAK1, signaling proteins downstream of DDR1 in PANC-1 cells; induces significant decrease of total protein levels of DDR1 and Bcl-xL, causes a significant reduction in the level of MMP-2 in NSCLS cells; suppresses the growth of K562 human CML cells with IC50 of 38 nM, A549, NCI-H23 and NCI-H460 human NSCLC cells with IC50 of 2.7, 2.1 and 3.0 µM, respectively; abrogates collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduces colony formation and migration, exhibits striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors.
PC-62396

ALW-II-49-7

1135219-23-6 ALW-II-49-7 (DDR2-IN-1) is a potent, selective DDR2 inhibitor with IC50 of 18.6 nM, also shows ability to inhibit DDR1 and Ephrin-family kinases (IC50=40 nM for EphB2); displays excellent overall kinase selectivity against a panel of over 350 kinases; decreases DDR2 phosphorylation but has little effect on the proliferation of DDR2 mutated cancer cell lines.

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