1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. ROS Kinase

ROS Kinase

The transmembrane proto-oncogene receptor tyrosine kinase (RTK) ROS is one of the last two remaining orphan receptor tyrosine kinases. Its normal expression pattern is tightly spatiotemporally restricted during development. The ectopic expression, as well as the production of variable mutant forms of ROS kinase, has been reported in a number of cancers, such as glioblastoma multiforme, and non-small cell lung cancer, suggesting a role for ROS kinase in deriving such tumors. It is thought also that the c-ROS gene may have a role in some cardiovascular diseases, and the fact that homozygous male mice targeted against the c-ROS gene are healthy but infertile has inspired researchers to think about ROS inhibition as a method for the development of new male contraceptives.

ROS1 is a transmembrane receptor tyrosine kinase proto-oncogene that has been shown to have rearrangements with several genes in glioblastoma, non-small-cell lung cancer (NSCLC), and other neoplasms, including intrachromosomal fusion with GOPC due to microdeletions at 6q22.1. ROS1 fusion events are important findings in these tumors, as they are potentially targetable alterations with newer tyrosine kinase inhibitors.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146038
    Antitumor agent-55
    Inducer
    Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3.
    Antitumor agent-55
  • HY-147866
    Antibacterial agent 110
    Inducer
    Antibacterial agent 110 (Compound 4e) is a potent antibacterial agent with a MIC value of 1 μg/mL against P. aeruginosa. Antibacterial agent 110 possesses favorable antibiofilm activity and can destroy cell membranes. Antibacterial agent 110 causes metabolic arrest and intracellular oxidative stress, and obstructs DNA replication.
    Antibacterial agent 110
  • HY-144255
    Antibacterial agent 70
    Antibacterial agent 70 is a new dihydropyrimidinone imidazole hybrid antibacterial agent, and its < b > MIC < / b > value is 0.5 μg/mL
    Antibacterial agent 70
  • HY-146399
    AChE/BChE-IN-9
    Inhibitor
    AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB.
    AChE/BChE-IN-9
  • HY-16229
    GGTI-2154
    Inhibitor
    GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.
    GGTI-2154
  • HY-148314
    ROS kinases-IN-2
    Inhibitor
    ROS kinases-IN-2 is a ROS kinase inhibitor with 21.53% inhibition at 10 μM.
    ROS kinases-IN-2
  • HY-N8724
    Lamalbid
    Lamalbid is a natural product that can be found in Lantana montevidensis. Lamalbid inhibits ROS generation.
    Lamalbid
  • HY-121397
    Phyltetralin
    Inhibitor
    Phyltetralin (Compound 10) is a natural product than can be isolated from the hexane-ethyl acetate extract of Phyllanthus amarus leaves. Phyltetralin possesses immunosuppressive effects on different lineages of innate immune system.
    Phyltetralin
  • HY-12678S1
    Entrectinib-d8
    Inhibitor
    Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.
    Entrectinib-d<sub>8</sub>
  • HY-153743
    Protein kinase inhibitor 4
    Inhibitor
    Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively).
    Protein kinase inhibitor 4
  • HY-147924
    Keap1-Nrf2-IN-11
    Inhibitor
    Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research.
    Keap1-Nrf2-IN-11
  • HY-150537
    AChE/GSK-3β-IN-1
    Inhibitor
    AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research.
    AChE/GSK-3β-IN-1
  • HY-147659
    AChE/BChE/BACE-1-IN-2
    Inhibitor
    AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-2
  • HY-146461
    Anticancer agent 58
    Activator
    Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model.
    Anticancer agent 58
  • HY-P4052
    Pinealon
    Inhibitor
    Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygen species (ROS) accumulation and suppresses the activation of ERK 1/2. Pinealon stimulates the functional activity of the main cellular elements of brain tissue, reduces the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia.
    Pinealon
  • HY-150571
    Anticancer agent 76
    Inducer
    Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis.
    Anticancer agent 76
  • HY-146462
    Anticancer agent 59
    Activator
    Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model.
    Anticancer agent 59
  • HY-157391
    ALK/ROS1-IN-3
    Inhibitor
    ALK/ROS1-IN-3 (compound C01) is a ROS1 and ALK dual inhibitor with IC50s of 42.3 nM and 49.1 nM for ROS1G2032R and ALKG1202R, respectively.
    ALK/ROS1-IN-3
  • HY-155405
    Anti-inflammatory agent 64
    Inhibitor
    Anti-inflammatory agent 64 (compound 4b) inhibits the secretion of IL-6 and TNF-α. Anti-inflammatory agent 64 has antioxidant and anti-inflammatory activity in vitro and in vivo. Anti-inflammatory agent 64 can effectively reduce paw edema .
    Anti-inflammatory agent 64
  • HY-16230
    GGTI-2417
    GGTI-2417 is a potent and selective inhibitor of GGTase I. GGTI-2417 inhibits the Cdk2-mediated phosphorylation of p27Kip1 at Thr187 and accumulates p27Kip1 in the nucleus. GGTI-2417 also induces breast cancer cell apoptosis.
    GGTI-2417
Cat. No. Product Name / Synonyms Application Reactivity