2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Discoidin Domain Receptor

Discoidin Domain Receptor

Discoidin Domain Receptor

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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:

Discoidin Domain Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162540
    LLC355
    		Degrader 99.71%
    LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader. LLC355 efficiently degrades DDR1 protein with a DC50 value of 150.8 nM in non-small cell lung cancer NCI-H23 cells. LLC355 induces DDR1 degradation via lysosome-mediated autophagy. LLC355 potently inhibits cancer cell tumorigenicity, migration, and invasion.
    LLC355
  • HY-15514A
    Merestinib dihydrochloride
    		Inhibitor 99.36%
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=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).
    Merestinib dihydrochloride
  • HY-133669
    DDR1-IN-5
    		Inhibitor 99.65%
    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-5
  • HY-13979A
    DDR1-IN-1 dihydrochloride
    		Inhibitor 98.92%
    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).
    DDR1-IN-1 dihydrochloride
  • HY-176184
    PROTAC DDR1 degrader-1
    		Degrader 98.69%
    PROTAC DDR1 degrader-1 is a PROTAC based DDR1 degrader (Red: DDR1 inhibitor (HY-176185), black: linker, Blue: E3 ligase ligand).
    PROTAC DDR1 degrader-1
  • HY-100695
    DDR-TRK-1
    		Inhibitor 98.90%
    DDR-TRK-1, a chemical probe, is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
    DDR-TRK-1
  • HY-167208
    SR-302
    		Inhibitor 98.51%
    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.
    SR-302
  • HY-RS03621
    Ddr1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Ddr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ddr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Ddr1 Mouse Pre-designed siRNA Set A
  • HY-NP131
    Recombinant Humanized Type III Collagen (10.4kDa)
    		Activator
    Recombinant Humanized Type III Collagen 10.4kDa is a novel biomaterial that have anticancer effects. Recombinant Humanized Type III Collagen 10.4kDa activates discoidin domain receptor 1 (DDR1), and thus inhibits autophagy, proliferation, and migration of cancer cells, and induces apoptosis.
    Recombinant Humanized Type III Collagen (10.4kDa)
  • HY-RS03620
    DDR1 Human Pre-designed siRNA Set A
    		Inhibitor

    DDR1 Human Pre-designed siRNA Set A contains three designed siRNAs for DDR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    DDR1 Human Pre-designed siRNA Set A
  • HY-RS03624
    Ddr2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Ddr2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ddr2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Ddr2 Mouse Pre-designed siRNA Set A
  • HY-RS03623
    DDR2 Human Pre-designed siRNA Set A
    		Inhibitor

    DDR2 Human Pre-designed siRNA Set A contains three designed siRNAs for DDR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    DDR2 Human Pre-designed siRNA Set A
  • HY-175202
    CIDD-8633
    		Inhibitor
    CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 inhibits cell migration and halts the cell cycle and induces apoptosis, significantly suppressing pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 can be used for the study of pancreatic cancer such as PDAC.
    CIDD-8633
  • HY-167745
    DDR1-IN-9
    		Inhibitor 99.64%
    DDR1-IN-9 is a selective inhibitor of DDR1 with significant kinase activity suppression, exhibiting a Kd value of 4.7 nM and an IC50 value of 9.4 nM. DDR1-IN-9 demonstrates reduced potency against a diverse panel of 400 nonmutated kinases, indicating its specificity. Additionally, DDR1-IN-9 shows favorable pharmacokinetic properties and potential therapeutic effects in a model of pulmonary fibrosis.
    DDR1-IN-9
  • HY-16961A
    Sitravatinib malate
    		Inhibitor
    Sitravatinib malate (MGCD516 malate) 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 malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
    Sitravatinib malate
  • HY-101034
    CHMFL-ABL/KIT-155
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
    CHMFL-ABL/KIT-155
  • HY-E70694
    DDR2 T654M Recombinant Human Active Protein Kinase
    Discoidin domain receptor 2 (DDR2) is a sensor for collagen and by participating in migration, proliferation, and extracellular matrix remodeling. DDR2 T654M is a DDR2 mutation. DDR2 T654M Recombinant Human Active Protein Kinase is a recombinant DDR2 T654M protein that can be used to study DDR2 T654M-related functions.
    DDR2 T654M Recombinant Human Active Protein Kinase
  • HY-169741
    DDR1-IN-10
    		Inhibitor
    DDR1-IN-10 (compound 7q) is a DDR1 inhibitor. DDR1-IN-10 can be used in the study of pancreatic cancer, non-small cell lung cancer, and gastric carcinoma.
    DDR1-IN-10
  • HY-153858
    PHI-501
    		Inhibitor
    PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.
    PHI-501
  • HY-179535
    Axl-IN-21
    		Inhibitor
    Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer[1] [2] .
    Axl-IN-21
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Discoidin Domain Receptor Isoform Comparison

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