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Results for "

activation loop

" in MedChemExpress (MCE) Product Catalog:

31

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4

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1

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3

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2

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2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101561
    Avapritinib
    10+ Cited Publications

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • HY-12795
    Vps34-IN-1
    Maximum Cited Publications
    15 Publications Verification

    		 PI3K Autophagy Cancer
    Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy .
    Vps34-IN-1
  • HY-W012078
    5-Methyl-2'-deoxycytidine
    3 Publications Verification

    5-Methyldeoxycytidine

    		 DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells .
    5-Methyl-2'-deoxycytidine
  • HY-P10373
    pJAK2(1001-1013)

    		JAK IFNAR Interleukin Related Infection Inflammation/Immunology
    pJAK2(1001-1013) is a cell-penetrating peptide that corresponds to the activation loop of JAK2 tyrosine kinase and functions as a SOCS1/3antagonist. pJAK2 (1001-1013) blocks SOCS1-mediated negative regulation of immune function, and enhances the biological activity of cytokines such as IFNγ and IL6. pJAK2(1001-1013) inhibits the replication of a broad range of viruses and exerts dose-dependent protective efficacy against lethal viral infections. pJAK2(1001-1013) can be used for the study of immune regulation and infection .
    pJAK2(1001-1013)
  • HY-124447
    BTYNB

    		IGF-1R c-Myc Apoptosis TGF-beta/Smad Cancer
    BTYNB is a structure-specific nucleic acid binder and IGF2BP1 inhibitor (with an IC50 of 5 μM against hBTYNB). BTYNB disrupts the IGF2BP1-RNA interaction and blocks its binding to oncogenic mRNAs such as c-Myc, MDM2, PD-L1. BTYNB completely blocks the INHBA-Smad2/3 pathway, disrupts the MYCN/IGF2BP1 loop, and thereby induces apoptosis and cell cycle arrest, effectively inhibiting the proliferation and survival of cancer cells. In addition, BTYNB acts as an immune activator and tumor microenvironment modulator, enhances T cell-mediated tumor killing, and produces significant synergistic effects with inhibitors of PD-1, BRD and BIRC5. BTYNB can be used in relevant research on various malignant tumors including ovarian cancer, neuroblastoma, leukemia and melanoma .
    BTYNB
  • HY-174801
    XL-3156

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    XL-3156 is a cGAS inhibitor. XL-3156 occupies both allosteric and orthosteric sites simultaneously, and inhibits the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of diseases such as autoimmune diseases and inflammation .
    XL-3156
  • HY-162080
    METTL1-WDR4-IN-1
    1 Publications Verification

    		 DNA Methyltransferase Pyruvate Kinase Cancer
    METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
    METTL1-WDR4-IN-1
  • HY-W740027
    5-Methyl-2'-deoxycytidine-d3

    5-Methyldeoxycytidine-d3

    		 Isotope-Labeled Compounds DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine-d3 (5-Methyldeoxycytidine-d3) is the deuterium labeled Methyl-2'-deoxycytidine (HY-W012078). 5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells .
    5-Methyl-2'-deoxycytidine-d3
  • HY-P1594A
    Dynorphin A (1-10) TFA

    		Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10) TFA
  • HY-174802
    XL-3158

    		Cyclic GMP-AMP Synthase IKK IFNAR Neurological Disease Inflammation/Immunology Cancer
    XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
    XL-3158
  • HY-P1594
    Dynorphin A (1-10)

    		Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10)
  • HY-174575
    Human MYOD1 mRNA

    		mRNA Cancer
    Human MYOD1 mRNA encodes the human myogenic differentiation 1 (MYOD1) protein, a nuclear protein that belongs to the basic helix-loop-helix family of transcription factors and the myogenic factors subfamily. MYOD1 acts as a transcriptional activator that promotes transcription of muscle-specific target genes and plays a role in muscle differentiation.
    Human MYOD1 mRNA
  • HY-E70746
    MEK1 SESE Recombinant Human Active Protein Kinase

    		MEK Cancer
    MEK1 is the MAP/ERK kinase. The MEK1 kinase directly phosphorylates ERK2, after the activation loop of MEK1 is itself phosphorylated by Raf. MEK1 SESE is a mutant of MEK1. MEK1 SESE Recombinant Human Active Protein Kinase is a recombinant MEK1 SESE protein that can be used to study MEK1 SESE-related functions .
    MEK1 SESE Recombinant Human Active Protein Kinase
  • HY-N10768
    1-Dehydro-[10]-gingerdione

    		IKK NF-κB Inflammation/Immunology
    1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research .
    1-Dehydro-[10]-gingerdione
  • HY-101561R
    Avapritinib (Standard)

    BLU-285 (Standard)

    		 Reference Standards c-Kit PDGFR Cancer
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib (Standard)
  • HY-W754911
    Avapritinib-d3

    BLU-285-d3

    		 Isotope-Labeled Compounds PDGFR c-Kit Cancer
    Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib-d3
  • HY-W012078R
    5-Methyl-2'-deoxycytidine (Standard)
    1 Publications Verification

    5-Methyldeoxycytidine (Standard)

    		 Reference Standards DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells .
    5-Methyl-2'-deoxycytidine (Standard)
  • HY-18849
    ERK2-IN-3

    		ERK Cancer
    ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
    ERK2-IN-3
  • HY-107458
    AP23848

    		c-Kit Cancer
    AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .
    AP23848
  • HY-174573
    Human NEUROD1 mRNA

    		mRNA Neurological Disease
    Human NEUROD1 mRNA encodes the human neuronal differentiation 1 (NEUROD1)protein, a member of the NeuroD family of basic helix-loop-helix (bHLH) transcription factors. NEUROD1 forms heterodimers with other bHLH proteins and activates transcription of genes that contain a specific DNA sequence known as the E-box.
    Human NEUROD1 mRNA
  • HY-E70744
    MEK1 F53L Recombinant Human Active Protein Kinase

    		MEK Cancer
    MEK1 is the MAP/ERK kinase. The MEK1 kinase directly phosphorylates ERK2, after the activation loop of MEK1 is itself phosphorylated by Raf. MEK1 F53L is a mutant of MEK1. MEK1 F53L Recombinant Human Active Protein Kinase is a recombinant MEK1 F53L protein that can be used to study MEK1 F53L-related functions .
    MEK1 F53L Recombinant Human Active Protein Kinase
  • HY-E70745
    MEK1 P124L Recombinant Human Active Protein Kinase

    		MEK Cancer
    MEK1 is the MAP/ERK kinase. The MEK1 kinase directly phosphorylates ERK2, after the activation loop of MEK1 is itself phosphorylated by Raf. MEK1 P124L is a mutant of MEK1. MEK1 P124L Recombinant Human Active Protein Kinase is a recombinant MEK1 P124L protein that can be used to study MEK1 P124L-related functions .
    MEK1 P124L Recombinant Human Active Protein Kinase
  • HY-176466
    ST-899

    		Platelet-activating Factor Receptor (PAFR) TNF Receptor Inflammation/Immunology
    ST-899 is a novel platelet-activating factor (PAF) receptor antagonist. ST-899 can significantly reduce the mortality of mice with endotoxin (LPS)-induced shock. ST-899 can significantly inhibit the increase in serum tumor necrosis factor (TNF) levels induced by LPS, but has no effect on interleukin-6 (IL-6). The regulatory mechanism of ST-899 is to block the positive feedback loop between PAF and TNF, thereby reducing the inflammatory response. ST-899 can be used to study inflammatory diseases such as septic shock .
    ST-899
  • HY-162080A
    METTL1-WDR4-IN-1 TFA
    1 Publications Verification

    		 DNA Methyltransferase Pyruvate Kinase Cancer
    METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
    METTL1-WDR4-IN-1 TFA
  • HY-E70807
    Biotin-WNK3 Recombinant Human Active Protein Kinase

    		WNK Kinase Neurological Disease
    WNK3 is a WNK kinase that associates with and activate SPAK/OSR1 by phosphorylation of its T-loop at Thr233 and Thr185. Biotin-WNK3 Recombinant Human Active Protein Kinase is obtained by expressing WNK3 proteins and is biotinylated .
    Biotin-WNK3 Recombinant Human Active Protein Kinase
  • HY-186167
    CDDO-biotin

    		IKK Cancer
    CDDO-biotin is an IKKβ inhibitor with cancer cell inhibitory activity. CDDO-biotin directly interacts with and oxidizes Cys-179 in the activation loop of IKKβ, forming an adduct with wild-type IKKβ. CDDO-biotin can be used in the research of myeloid leukemia, osteosarcoma, multiple myeloma, lung cancer, breast cancer and pancreatic cancer .
    CDDO-biotin
  • HY-P992456
    SAR-443809

    		Complement System Cardiovascular Disease Endocrinology
    SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway .
    SAR-443809
  • HY-182430
    NVP-BVB808

    		JAK STAT Apoptosis Cancer
    NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia .
    NVP-BVB808
  • HY-P11797
    EP9

    		Transmembrane Glycoprotein Cardiovascular Disease
    EP9 is a 7-amino acid peptide targeting CD63. EP9 binds specifically to the extracellular region of CD63, including a groove in the large extracellular loop (EC2) or the extracellular end of CD63’s central cavity, triggering endocytosis of decorated nanoemulsions/liposomes into cells. EP9 promotes cellular uptake of decorated nanoemulsions/liposomes into activated cardiac fibroblasts and epicardial stromal cells via caveolae and/or clathrin-coated pits. EP9 can be used for the research of myocardial infarction, cardiac fibrosis .
    EP9
  • HY-183554
    Fa-Au

    		TrxR Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS) IFNAR STAT Cancer
    Fa-Au is a TrxR inhibitor. Fa-Au downregulates GPX4, induces oxidative stress, mitochondria-associated ferroptosis (ferroptosis) and immunogenic cell death. Fa-Au induces ROS production in hepatoma cells. Fa-Au remodels the tumor immune microenvironment via M1 macrophage polarization, dendritic cell maturation, CD8+ T cell activation and reduction of regulatory T cells. Fa-Au induces an anti-tumor immune feedback loop through the IFNγ/STAT1/SLC7A11 axis. Fa-Au inhibits tumor growth. Fa-Au is applicable to hepatocellular carcinoma-related research .
    Fa-Au
  • HY-46286
    TTFB

    N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide

    		 5-HT Receptor nAChR GABA Receptor Glycine Receptor (GlyR) Neurological Disease
    TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn 2+- and H +-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
    TTFB

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