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-16229A
    GGTI-2154 hydrochloride
    		Inhibitor 98.93%
    GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer.
    GGTI-2154 hydrochloride
  • HY-N1318
    Salvigenin
    		Inhibitor 99.82%
    Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties. Salvigenin inhibits H2O2-induced cell apoptosis.
    Salvigenin
  • HY-149394
    PRDX1-IN-1
    		98.04%
    PRDX1-IN-1 is a selective inhibtor of PRDX1 with an IC50 value of 0.164 μM. PRDX1-IN-1 can be used in researches related to cancer.PRDX1-IN-1 promots intracellular ROS accumulation, and inhibits the proliferation, invasion and migration of cancer cells besides inducing apoptosis. PRDX1-IN-1 could be used in cancer research.
    PRDX1-IN-1
  • HY-50878S
    Crizotinib-d5
    		Inhibitor ≥99.0%
    Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib-d<sub>5</sub>
  • HY-15514A
    Merestinib dihydrochloride
    		Inhibitor 99.36%
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
    Merestinib dihydrochloride
  • HY-155163
    APG-2449
    		Inhibitor 98.86%
    APG-2449 is an orally active ALK/ROS1/FAK inhibitor. APG-2449 shows antitumor activity in mouse models of non-small cell lung cancer (NSCLC).
    APG-2449
  • HY-112801
    F-1
    		Inhibitor 98.65%
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
    F-1
  • HY-W402148
    10-Methyl-9-(phenoxycarbonyl)acridinium (fluorosulfonate)
    		99.79%
    10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate, a phenyl ester of acridinium esters, is a fluorescent dye that produces chemiluminescent under neutral conditions. 10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate can be used for the measurement of hydrogen peroxide.
    10-Methyl-9-(phenoxycarbonyl)acridinium (fluorosulfonate)
  • HY-125711
    Capsanthin
    		Inhibitor
    Capsanthin is a carotenoid that has been found in C. annuum. Capsanthin has antioxidant、antitumor and anti-inflammatory effects.
    Capsanthin
  • HY-148228
    ROS kinases-IN-1
    		Inhibitor 98.30%
    ROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity.
    ROS kinases-IN-1
  • HY-131003A
    Taletrectinib free base
    		Inhibitor
    Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
    Taletrectinib free base
  • HY-111416
    WY-135
    		Inhibitor
    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
    WY-135
  • HY-147658
    AChE/BChE/BACE-1-IN-1
    		Inhibitor
    AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 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-1 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-1
  • HY-146432
    Antitumor agent-60
    		Activator
    Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model.
    Antitumor agent-60
  • HY-144252
    Antibacterial agent 69
    Antimicrobial agent 69 is a novel structural antimicrobial regulator and has been used to fight deadly multidrug-resistant bacterial infections, and its < b > MICs < / b > value is 2.978 μM。
    Antibacterial agent 69
  • HY-120229
    GGTI-2147
    		Inhibitor
    GGTI-2147 is a potent GGTase I inhibitor. GGTI-2147 blocks geranyl-geranylation of Rap1A and reduces the activity of Rac1 (one of substrates for GGTI) and ameliorates the OGD/R-induced neuronal apoptosis.GGTI-2147 can be used for neurodevelopmental disorders research, such as autism, depression, and schizophrenia.
    GGTI-2147
  • 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
Cat. No. Product Name / Synonyms Application Reactivity