1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor

Discoidin Domain Receptor (盘状结构域受体)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101034
    CHMFL-ABL/KIT-155
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的,具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM),对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。
    CHMFL-ABL/KIT-155
  • HY-14979A
    ML786 dihydrochloride Inhibitor
    ML786 dihydrochloride 是一种有效和具有口服活性的 Raf 抑制剂,对 V600EΔB-Rafwt B-RafC-RafIC50 值分别为2.1,4.2 和 2.5 nM。ML786 dihydrochloride 还抑制 Abl-1DDR2EPHA2VEGFR2/KDR/Flk-1RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM)。ML786 dihydrochloride 可用于癌症研究。
    ML786 dihydrochloride
  • HY-160689
    GW694590A Inhibitor
    GW694590A (UNC10112731) 是 MYC 蛋白稳定剂,能够增加内源性 MYC 蛋白的水平。GW694590A 还靶向受体酪氨酸激酶,在 1 μM 时,对 DDR2KITPDGFRα 的抑制率分别为 81%、68% 和 67%。GW694590A 是跨 ATP 依赖性和非依赖性荧光素酶的蛋白激酶抑制剂,对 Fluc 报告基因有潜在影响。
    GW694590A
  • HY-150552
    JNK3 inhibitor-2
    JNK3 inhibitor-2 是一种有效的选择性 JNK3 抑制剂,对于 JNK1、JNK2、 JNK3的 IC50 值分别为 >100, >100, 0.25 µM。JNK3 inhibitor-2 显示出对 DDR1EGFR (T790M, L858R) 的抑制作用。
    JNK3 inhibitor-2
  • HY-162102
    DDR1-IN-8 Inhibitor
    DDR1-IN-8 (compound 7s) 是一种有效的 DDR1/2 抑制剂,IC50 值分别为 0.045 μM 和 0.126 μM,DDR1-IN-8 具有抗肿瘤活性。
    DDR1-IN-8
  • HY-W778154
    O,O-Dimethyl dithiophosphate-13C2 ammonium Inhibitor
    O,O-Dimethyl dithiophosphate-13C2 (ammonium) 是 O,O-Dimethyl dithiophosphate-13C2 (ammonium) 的 13C 标记的同位素。
    O,O-Dimethyl dithiophosphate-<sup>13</sup>C<sub>2</sub> ammonium
  • HY-13979A
    DDR1-IN-1 dihydrochloride Inhibitor
    DDR1-IN-1 dihydrochloride是DDR1受体酪氨酸激酶抑制剂,IC50 值为105 nM,而对 DDR2 的 IC50 为413 nM。
    DDR1-IN-1 dihydrochloride
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