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-16961
    Sitravatinib
    		Inhibitor 99.59%
    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/Flt-4, VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, 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.
    Sitravatinib
  • HY-13979
    DDR1-IN-1
    		Inhibitor 98.20%
    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).
    DDR1-IN-1
  • HY-U00444
    7rh
    		Inhibitor 99.54%
    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.
    7rh
  • HY-15514
    Merestinib
    		Inhibitor 99.99%
    Merestinib (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).
    Merestinib
  • HY-114169
    WRG-28
    		Inhibitor 99.34%
    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.
    WRG-28
  • 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-135401
    VU6015929
    		Inhibitor 99.26%
    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.
    VU6015929
  • HY-100756
    BAY-826
    		Inhibitor 99.94%
    BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.
    BAY-826
  • HY-133670
    DDR1-IN-6
    		Inhibitor 98.16%
    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.
    DDR1-IN-6
  • HY-114311
    FGFR1/DDR2 inhibitor 1
    		Inhibitor 98.26%
    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.
    FGFR1/DDR2 inhibitor 1
  • HY-114173
    DDR1-IN-4
    		Inhibitor 98.01%
    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.
    DDR1-IN-4
  • HY-W018931
    DDR Inhibitor
    		Inhibitor 99.47%
    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.
    DDR Inhibitor
  • 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 99.27%
    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-112545
    DDR2-IN-1
    		Inhibitor 99.88%
    DDR2-IN-1 is potent DDR2 inhibitor with an IC50 of 26 nM. DDR2-IN-1, compound 129, can be used for osteoarthritis research.
    DDR2-IN-1
  • 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/Flt-4, VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, 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-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-156552
    DDR1/2 inhibitor-2
    		Inhibitor
    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.
    DDR1/2 inhibitor-2
  • 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, VEGFR2/KDR/Flk-1, 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-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
Cat. No. Product Name / Synonyms Species Source
Discoidin Domain Receptor Isoform Comparison

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