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-P990400
    Anti-DDR1/CD167a Antibody
    		Inhibitor 99.13%
    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-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-183068
    AP4-43
    		Inhibitor
    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.
    AP4-43
  • HY-181839
    DDR1/2 IN-4
    		Inhibitor
    DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis.
    DDR1/2 IN-4
  • HY-172797
    DDR Inhibitor 2
    		Inhibitor
    DDR Inhibitor 2 (compound 5a) is a discoidin domain receptor (DDR) inhibitor with an IC50 of 0.125 μM. DDR Inhibitor 2 can be used for study of fibrotic diseases.
    DDR Inhibitor 2
  • HY-176849
    DDR2-IN-2
    		Inhibitor
    DDR2-IN-2 is a Discoidin domain receptor 2 (DDR2) inhibitor. DDR2-IN-2 can be used for the research of cancer.
    DDR2-IN-2
  • 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-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-14979
    ML786
    		Inhibitor
    ML786 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 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.
    ML786
  • HY-114510
    PRMT/HKMT-IN-1
    		Inhibitor
    PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia.
    PRMT/HKMT-IN-1
  • HY-E70693
    DDR2 N456S 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 N456S is a DDR2 mutation that may be present in non-small cell lung cancer. DDR2 N456S Recombinant Human Active Protein Kinase is a recombinant DDR2 N456S protein that can be used to study DDR2 N456S-related functions.
    DDR2 N456S Recombinant Human Active Protein Kinase
  • HY-150552
    JNK3 inhibitor-2
    JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100, >100, 0.25 µM for JNK1, JNK2, JNK3, respectively. JNK3 inhibitor-2 shows DDR1 and EGFR (T790M, L858R) inhibition.
    JNK3 inhibitor-2
  • HY-162102
    DDR1-IN-8
    		Inhibitor
    DDR1-IN-8 (compound 7s) is a potent inhibitor of DDR1/2, with the IC50 values of 0.045 μM and 0.126 μM, respectively. DDR1-IN-8 has anti-tumor activity.
    DDR1-IN-8
  • HY-122848
    DDR1/2 inhibitor-3
    		Inhibitor
    DDR1/2 inhibitor-3 (5n) is a DDR1/2 inhibitor, with IC50 values​of 9.4 and 20.4 nM, respectively. DDR1/2 inhibitor-3 can be used in anti-inflammatory research.
    DDR1/2 inhibitor-3
  • HY-W778154
    O,O-Dimethyl dithiophosphate-13C2 ammonium
    		Inhibitor
    O,O-Dimethyl dithiophosphate-13C2 ammonium is the 13C labeled isotope of O,O-Dimethyl dithiophosphate ammonium.
    O,O-Dimethyl dithiophosphate-<sup>13</sup>C<sub>2</sub> ammonium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Discoidin Domain Receptor Isoform Comparison

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