- Signaling Pathways
- Protein Tyrosine Kinase/RTK
- 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.
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ROS Kinase Related Products (101)
Related Products (101)
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Antibodies (3)
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Antibacterial agent 110
0 ImagesCat. No.: HY-147866CAS No.: 3033492-79-1Antibacterial 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. -
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Higenamine-d4 hydrochloride
0 ImagesCat. No.: HY-N2037ASCAS No.: 2249814-84-2Synonyms: Norcoclaurine-d4 hydrochloride; Demethyl-Coclaurine-d4 hydrochlorideHigenamine-d4 (Norcoclaurine-d4; Demethyl-Coclaurine-d4) hydrochloride is deuterium-labeled Higenamine (hydrochloride) (HY-N2037A). -
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AChE/BChE-IN-9
0 ImagesCat. No.: HY-146399CAS No.: 2761542-55-4AChE/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. -
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SMU-B
0 ImagesCat. No.: HY-120387CAS No.: 1253286-90-6SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models. -
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Lamalbid
0 ImagesCat. No.: HY-N8724CAS No.: 52212-87-0Lamalbid is a natural product that can be found in Lantana montevidensis. Lamalbid inhibits ROS generation. -
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Phyltetralin
0 ImagesCat. No.: HY-121397CAS No.: 123048-17-9Phyltetralin (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. -
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Protein kinase inhibitor 4
0 ImagesCat. No.: HY-153743CAS No.: 2278205-04-0Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively). -
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Keap1-Nrf2-IN-11
0 ImagesCat. No.: HY-147924CAS No.: 2796292-75-4Keap1-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. -
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AChE/GSK-3β-IN-1
0 ImagesCat. No.: HY-150537CAS No.: 2412364-73-7AChE/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. -
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Kukoamine B-d5 dihydrochloride
0 ImagesCat. No.: HY-N2393SKukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis. . -
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Kukoamine B (Standard)
0 ImagesCat. No.: HY-N2393RCAS No.: 164991-67-7Kukoamine B (Standard) is the analytical standard of Kukoamine B. This product is intended for research and analytical applications. Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis. -
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AChE/BChE/BACE-1-IN-2
0 ImagesCat. No.: HY-147659CAS No.: 1877000-20-8AChE/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. -
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Anticancer agent 58
0 ImagesCat. No.: HY-146461Anticancer 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. -
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SMU-037
0 ImagesCat. No.: HY-178391SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research. -
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Anticancer agent 76
0 ImagesCat. No.: HY-150571CAS No.: 2448091-11-8Anticancer 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. -
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ALK/ROS1-IN-5
0 ImagesCat. No.: HY-170418ALK/ROS1-IN-5 (compound X4) is a selective ALK and ROS1 kinases inhibitor with IC50s of 0.512 μM (ALK), 0.766 μM (ROS1), respectively. ALK/ROS1-IN-5 inhibits H2228 cells with an IC50 of 0.034 μM. ALK/ROS1-IN-5 induces cancer cells apoptosis in dose-dependent manner. ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells[1]. -
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Anticancer agent 59
0 ImagesCat. No.: HY-146462CAS No.: 2366170-11-6Anticancer 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. -
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Topo I/II-IN-2
0 ImagesCat. No.: HY-170912Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. . -
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- ALK/ROS1-IN-3
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Anti-inflammatory agent 64
0 ImagesCat. No.: HY-155405CAS No.: 3016401-76-3Anti-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 . -
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