Discoidin Domain Receptor Inhibitor

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC₅₀ of 105 nM; 4-fold less potent for DDR2 (IC₅₀ = 413 nM).

7rh (DDR1-IN-2) is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC₅₀ of 13.1 nM, and also less potently inhibits DDR2, with an IC₅₀ of 203 nM. 7rh is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC₅₀ values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.

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.

AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor. AP4-43 reduces growth of mammalian colorectal cancer organoids. AP4-43 improves survival in a transgenic Drosophila model of KRAS-mutant colorectal cancer. AP4-43 can be used for the research of KRAS-mutant colorectal cancer.

Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis.

Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (K_i=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC₅₀=11 nM), FLT3 (IC₅₀=7 nM), AXL (IC₅₀=2 nM), MERTK (IC₅₀=10 nM), TEK (IC₅₀=63 nM), ROS1, DDR1/2 (IC₅₀=0.1/7 nM) and MKNK1/2 (IC₅₀=7 nM).

BAY-826, a chemical probe, is a selective and potent TIE-2 inhibitor with a K_d of 1.6 nM, respectively.

VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC₅₀s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.

DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC₅₀ values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

DDR2-IN-1 is potent DDR2 inhibitor with an IC₅₀ of 26 nM. DDR2-IN-1, compound 129, can be used for osteoarthritis research.

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC₅₀ values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.

DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC₅₀ of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC₅₀ of 9.7 nM. DDR1-IN-6 has anti-cancer activity. DDR1-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC₅₀ of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.

DDR1/2 inhibitor-2 (Example 31) is a DDR1/DDR2 inhibitor, with IC₅₀ values less than 100 nM. DDR1/2 inhibitor-2 can be used for research of cancer and fibrotic diseases.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (K_i=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC₅₀=11 nM), FLT3 (IC₅₀=7 nM), AXL (IC₅₀=2 nM), MERTK (IC₅₀=10 nM), TEK (IC₅₀=63 nM), ROS1, DDR1/2 (IC₅₀=0.1/7 nM) and MKNK1/2 (IC₅₀=7 nM).

DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC₅₀ of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC₅₀ of 4.1 nM. DDR1-IN-5 has anti-cancer activity. DDR1-IN-5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC₅₀ of 105 nM; 4-fold less potent for DDR2 (IC₅₀ = 413 nM).

SR-302, a chemical probe, is a potent and selectivity DDR/p38 inhibitor, with IC₅₀ values of 0.125, 0.023 and 0.018 μM for p38α, DDR1 and DDR2, respectively. SR-302 can be used for the research of fibrotic disorders, such as renal and pulmonary fibrosis, atherosclerosis, and various forms of cancer.