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-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-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-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-13979A
    DDR1-IN-1 dihydrochloride
    		Inhibitor
    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-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-P990400
    Anti-DDR1/CD167a Antibody
    		Inhibitor
    Anti-DDR1/CD167a Antibody is a CHO-expressed antibody that targets DDR1/CD167a. The Anti-DDR1/CD167a Antibody has a mouse IgG1 type heavy chain and a mouse κ type light chain, with a predicted molecular weight (MW) of 143.32 kDa. The isotype control for Anti-DDR1/CD167a Antibody can refer to Mouse IgG1 kappa, Isotype Control (HY-P99977).
    Anti-DDR1/CD167a Antibody
  • HY-162540
    LLC355
    		Degrader
    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-14979A
    ML786 dihydrochloride
    		Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • 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-176849
    DDR1-IN-12
    		Inhibitor
    DDR1-IN-12 (Compound 7t) is a highly selective discoidin domain receptor 1 (DDR1) inhibitor (IC50=0.126 μM). DDR1-IN-12 blocks receptor tyrosine kinase autophosphorylation and downstream signaling (e.g., inhibition of TGF-β1-induced fibroblast activation), inhibiting tumor cell migration and pulmonary fibrosis progression. DDR1-IN-12 is promising for research of lung cancer (especially lung adenocarcinoma).
    DDR1-IN-12
  • HY-175281
    SJ11646
    		Degrader
    SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
    SJ11646
  • HY-160689
    GW694590A
    		Inhibitor
    GW694590A (UNC10112731) is a MYC protein stabilizer that increases endogenous MYC protein levels. GW694590A also targets receptor tyrosine kinases, inhibiting DDR2, KIT and PDGFRα by 81% at 1 μM. , 68% and 67%. GW694590A is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential effects on the Fluc reporter gene.
    GW694590A
  • HY-167208
    SR-302
    		Inhibitor
    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-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-173284
    DDR1-IN-11
    		Inhibitor
    DDR1-IN-11 (Compound 4) is an inhibitor of Discoidin domain receptor 1 (DDR1) with an IC50 of 46.16 nM. DDR1-IN-11 can achieve an inhibition rate of 99.86% against Z-138 cells at a concentration of 10 μM, and it can be used in the research of acute myeloid leukemia (AML).
    DDR1-IN-11
  • HY-P991683
    Ensavatatug
    		Inhibitor
    Ensavatatug is a humanized monoclonal antibody inhibitor targeting discoidin domain receptor tyrosine kinase 1 (DDR1). Ensavatatug is promising for research of cancers.
    Ensavatatug
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Discoidin Domain Receptor Isoform Comparison

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