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-152292
    Zidesamtinib
    		Inhibitor 99.55%
    Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.
    Zidesamtinib
  • HY-145574
    Iruplinalkib
    		Inhibitor 99.62%
    Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer.
    Iruplinalkib
  • HY-N1318
    Salvigenin
    		Inhibitor 99.93%
    Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties. Salvigenin inhibits H2O2-induced cell apoptosis.
    Salvigenin
  • HY-N2037
    Higenamine
    		Inhibitor 98.91%
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
    Higenamine
  • HY-B0873
    Uniconazole
    		Inhibitor 99.68%
    Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent.
    Uniconazole
  • HY-12678S1
    Entrectinib-d8
    		Inhibitor 99.82%
    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-155163
    APG-2449
    		Inhibitor 98.93%
    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-Y1117
    Melamine
    		Activator 99.17%
    Melamine is an orally active inducer of Apoptosis. Melamine induces animal disease models. Melamine affects the activity of Sertoli cell and can be used for research on male reproductive function. Melamine also has neurotoxicity and nephrotoxicity. Melamine induces cognitive impairment and acute kidney injury models. Melamine can also be used to induce bladder cancer and urinary stone models.
    Melamine
  • HY-50878S
    Crizotinib-d5
    		Inhibitor 99.60%
    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-17437
    Mefloquine
    		Inducer 99.96%
    Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.
    Mefloquine
  • HY-13326
    ASP3026
    		99.88%
    ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.
    ASP3026
  • HY-P4052
    Pinealon
    		Inhibitor 99.34%
    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-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-16230
    GGTI-2417
    		98.97%
    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
  • HY-112801
    F-1
    		Inhibitor 98.03%
    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-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-N0394R
    L-Cystine (Standard)
    		Inhibitor
    L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis
    L-Cystine (Standard)
  • HY-N0416R
    Cucurbitacin B (Standard)
    		Inhibitor
    Cucurbitacin B (Standard) is the analytical standard of Cucurbitacin B. This product is intended for research and analytical applications. Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.
    Cucurbitacin B (Standard)
  • 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-D0885D
    Phosphocreatine disodium hydrate
    		Inhibitor 99.57%
    Phosphocreatine (disodium hydrate) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine (disodium hydrate) enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine (disodium hydrate) normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine (disodium hydrate) Phosphocreatine (disodium hydrate) provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway..
    Phosphocreatine disodium hydrate
Cat. No. Product Name / Synonyms Application Reactivity