2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Discoidin Domain Receptor
  5. DDR1 Isoform

DDR1

 
Cat. No. Product Name Effect Purity
  • HY-16961
    Sitravatinib
    		Inhibitor 99.57%
    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, VEGFR2, VEGFR1, 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.
  • HY-157442
    GLPG3312
    		Inhibitor 98.63%
    GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
  • HY-135401
    VU6015929
    		Inhibitor 99.50%
    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.
  • HY-114173
    DDR1-IN-4
    		Inhibitor 98.19%
    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.
  • HY-NP175
    Collagen (bovine skin)
    		Ligand
    Collagen (bovine skin) is a three-dimensional cell culture matrix and morphoregulator extracted from bovine skin, which binds to integrins (such as α1β1, α2β1, α11β1) and discoidin domain receptors (DDR1 and DDR2). Collagen (bovine skin) can be reconstituted into a three-dimensional fibrous network to mimic the in vivo tissue environment. It can not only be modified through cross-linking or concentration adjustment, but also interact with fibronectin to enhance matrix-associated cellular activities. Collagen (bovine skin) mediates the proliferation, aggregation, durotactic migration and differentiation of fibroblasts, regulates the synthesis, remodeling and contraction of extracellular matrix, and modulates the expression, activation of MMP as well as cell apoptosis, etc. Collagen (bovine skin) can be used in studies related to the mechanisms of cancer occurrence and development.
  • 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] .
  • 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.
  • 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.
  • HY-133670
    DDR1-IN-6
    		Inhibitor 98.02%
    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.
  • HY-156552
    DDR1/2 inhibitor-2
    		Inhibitor 99.73%
    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.
  • 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.
  • 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).
  • 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.
  • 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.
  • 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)
  • 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).
  • 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.
  • 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.
Cat. No. Product Name / Synonyms Species Source