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Home >> Signaling Pathways >> Tyrosine Kinase >> Discoidin Domain Receptor

Discoidin Domain Receptor

Discoidin domain receptors (DDRs) are receptor tyrosine kinases with the unique ability among receptor tyrosine kinases to respond to collagen. Several signaling molecules have been implicated in DDR signaling, including Shp-2, Src, and MAPK pathways. DDRs have been reported to induce the expression of various genes including matrix metalloproteinases and bone morphogenetic proteins, but the regulatory mechanisms underlying DDR-induced gene expression remain to be determined. DDRs regulate cell-collagen interactions in normal and pathological conditions and thus are emerging as major sensors of collagen matrices and potential novel therapeutic targets.

Targets for  Discoidin Domain Receptor

Products for  Discoidin Domain Receptor

  1. Cat.No. Product Name Information
  2. GC33361 DDR Inhibitor 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 Chemical Structure
  3. GC17365 DDR1-IN-1 selective DDR1 receptor tyrosine kinase inhibitor DDR1-IN-1 Chemical Structure
  4. GC35822 DDR1-IN-1 dihydrochloride 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 Chemical Structure
  5. GC31724 DDR1-IN-2

    7rh

     DDR1-IN-2 (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. DDR1-IN-2 Chemical Structure
  6. GC33297 DDR1-IN-3 DDR1-IN-3 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR1-IN-3 also inhibits TRK family. DDR1-IN-3 Chemical Structure
  7. GC64268 DDR1-IN-4 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 Chemical Structure
  8. GC65378 DDR1-IN-5 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 Chemical Structure
  9. GC66476 DDR1-IN-6 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 Chemical Structure
  10. GC73659 DDR1/2 inhibitor-2 DDR1/2 inhibitor-2 (Example 31) is a DDR1/DDR2 inhibitor, with IC50 values less than 100 nM. DDR1/2 inhibitor-2 Chemical Structure
  11. GC70345 DDR2-IN-1 DDR2-IN-1 is potent DDR2 inhibitor with an IC50 of 26 nM. DDR2-IN-1 Chemical Structure
  12. GC65212 FGFR1/DDR2 inhibitor 1 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 Chemical Structure
  13. GC11057 LY2801653

    Merestinib

     A MET kinase inhibitor LY2801653 Chemical Structure
  14. GC36585 Merestinib dihydrochloride 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 Chemical Structure
  15. GC19332 Sitravatinib

    MGCD-516

     Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth with IC50 of 3980 nmol/L. Sitravatinib Chemical Structure
  16. GC39301 VU6015929 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 Chemical Structure
  17. GC38206 WRG-28 WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 Chemical Structure

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