Discoidin Domain Receptor
Discoidin domain receptors (DDRs) are members of the transmembrane receptor tyrosine kinase (RTK) superfamily which are distinguished from others by the presence of a discoidin motif in the extracellular domain and their utilization of collagens as internal ligands. Two types of DDRs, DDR1 and DDR2, have been identified with distinct expression profiles and ligand specificities.
Upon collagen binding, DDRs transduce cellular signaling involved in various cell functions, including cell adhesion, proliferation, differentiation, migration, and matrix homeostasis. Altered DDR function resulting from either mutations or overexpression has been implicated in several types of disease, including atherosclerosis, inflammation, cancer, and tissue fibrosis. DDRs have been considered as novel potential molecular targets for drug discovery and increasing efforts are being devoted to the identification of new small molecule inhibitors targeting the receptors.
Discoidin Domain Receptor Isoform Specific Products
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Discoidin Domain Receptor Inhibitors
(45)
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Discoidin Domain Receptor Activator
(1)
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Discoidin Domain Receptor Modulators
(2)
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Discoidin Domain Receptor Degraders
(3)
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Discoidin Domain Receptor Ligands
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DDR1/CD167a Proteins
(12)
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DDR2 Proteins
(10)
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Discoidin Domain Receptor Related Products (59)
Related Products (59)
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Recombinant Proteins (22)
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Antibodies (1)
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Discoidin Domain Receptor Isoform Comparison
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7rh
0 ImagesSynonyms: DDR1-IN-27rh (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.
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Sitravatinib
0 ImagesSynonyms: MGCD516; MG-516Sitravatinib (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.
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GLPG3312
0 ImagesGLPG3312 (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.
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WRG-28
0 ImagesWRG-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.
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AP4-43
0 ImagesCat. No.: HY-183068Purity: 99.76%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.
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Anti-Mouse DDR2 Antibody (DAB0065)
0 ImagesCat. No.: HY-P992066Anti-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.
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Merestinib
0 ImagesSynonyms: LY2801653Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=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).
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Recombinant Humanized Type III Collagen 28.6kDa
0 ImagesCat. No.: HY-NP132Recombinant Humanized Type III Collagen 28.6kDa is a 28.6 kDa recombinant humanized type III collagen. Recombinant Humanized Type III Collagen possesses a variety of biological functions, such as promoting the regeneration of the skin extracellular matrix and improving the cellular microenvironment. Recombinant Humanized Type III Collagen can also inhibit the proliferation, migration and invasion of breast cancer cells. Recombinant Humanized Type III Collagen plays a role in cell adhesion, migration, proliferation and differentiation by interacting with Integrin.
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VU6015929
0 ImagesVU6015929 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.
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Recombinant humanized type III collagen (MW 55900)
0 ImagesCat. No.: HY-NP132ARecombinant humanized type III collagen (MW 55900) is a type III collagen with a molecular weight of 55900 Da. Recombinant humanized type III collagen has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. Recombinant humanized type III collagen inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins.
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DDR1-IN-4
0 ImagesDDR1-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.
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Collagen (bovine skin)
0 ImagesCollagen (bovine skin) is a three-dimensional cell culture matrix and morphoregulator extracted from bovine skin, which binds to integrins (such as α1β1, α2β1, α11β1) and discoidin domain receptors (DDR1 and DDR2). Collagen (bovine skin) can be reconstituted into a three-dimensional fibrous network to mimic the in vivo tissue environment. It can not only be modified through cross-linking or concentration adjustment, but also interact with fibronectin to enhance matrix-associated cellular activities. Collagen (bovine skin) mediates the proliferation, aggregation, durotactic migration and differentiation of fibroblasts, regulates the synthesis, remodeling and contraction of extracellular matrix, and modulates the expression, activation of MMP as well as cell apoptosis, etc. Collagen (bovine skin) can be used in studies related to the mechanisms of cancer occurrence and development.
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FGFR1/DDR2 inhibitor 1
0 ImagesFGFR1/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.
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DDR1-IN-6
0 ImagesDDR1-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.
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DDR Inhibitor
0 ImagesDDR 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.
