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

ROS Kinase

ROS Kinase

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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-157084
    HS-291
    		Activator
    HS-291 is a HtpG inhibitor of Borrelia burgdorferi (Bb). HS-291 contains BX-2819 (high affinity for Bb HtpG), PEG linker, and Verteporfin (HY-B0146) (a photoactive toxin).HS-291 produces reactive oxygen species under light activation to oxidize HtpG and a discrete protein subset near chaperone proteins and can quickly and irreversibly inactivate Bb.
    HS-291
  • HY-130794
    ALK/ROS1-IN-1
    		Inhibitor
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
    ALK/ROS1-IN-1
  • HY-150974
    ROS1-IN-1
    		Inhibitor
    ROS1-IN-1 (Compound 31) is a potent and selective ROS1 kinase inhibitor with an IC50 of 0.097 μM.
    ROS1-IN-1
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity