Cayman

Showing 8701–8850 of 45550 results

  • AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis.{41747,41745,41746} It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC90s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.{41747}  

     

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    Cayman
    SKU:24686 - 10 mg

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  • AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis.{41747,41745,41746} It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC90s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.{41747}  

     

    Brand:
    Cayman
    SKU:24686 - 25 mg

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  • AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis.{41747,41745,41746} It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC90s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.{41747}  

     

    Brand:
    Cayman
    SKU:24686 - 5 mg

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  • Afobazole is a multi-targeted anxiolytic drug with neuroprotective activities.{46420,46421} It binds to the sigma-1, melatonin MT1, and MT3 receptors, as well as monoamine oxidase A (MAO-A; Kis = 5.9, 160, 0.97, and 3.6 µM, respectively, in a radioligand binding assay).{46420} Afobazole (5 mg/kg) decreases the latency to enter, as well as increases the number of entries into and percentage of time spent in, the open arms of the elevated plus maze, indicating anxiolytic-like activity in passive stress-coping BALB/c, but not active stress-coping C57BL/6, mice.{46422} It decreases stroke volume and neuronal and oligodendroglial cell death in the brain in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at doses of 0.3 and 3 mg/kg.{46421}  

     

    Brand:
    Cayman
    SKU:22923 - 1 mg

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  • Afobazole is a multi-targeted anxiolytic drug with neuroprotective activities.{46420,46421} It binds to the sigma-1, melatonin MT1, and MT3 receptors, as well as monoamine oxidase A (MAO-A; Kis = 5.9, 160, 0.97, and 3.6 µM, respectively, in a radioligand binding assay).{46420} Afobazole (5 mg/kg) decreases the latency to enter, as well as increases the number of entries into and percentage of time spent in, the open arms of the elevated plus maze, indicating anxiolytic-like activity in passive stress-coping BALB/c, but not active stress-coping C57BL/6, mice.{46422} It decreases stroke volume and neuronal and oligodendroglial cell death in the brain in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at doses of 0.3 and 3 mg/kg.{46421}  

     

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    Cayman
    SKU:22923 - 5 mg

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  • Prostaglandin I2 is an unstable prostanoid which, through the ‘I prostanoid’ (IP) receptor, inhibits platelet aggregation and promotes vasodilatation in pulmonary vascular beds. AFP 07 is a 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki = 0.561 nM).{7236} AFP 07 shows weaker affinity for EP receptors, with Ki values of > 100 nM for EP1-3 and > 10 nM for EP4.{7236} In piglet and rabbit saphenous veins, which express both IP and EP4, the EP4 antagonist AH 23848 reduces AFP 07-mediated relaxation, suggesting that AFP 07 activates EP4 as well as IP, particularly when both receptors are present.{15488}  

     

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  • Prostaglandin I2 is an unstable prostanoid which, through the ‘I prostanoid’ (IP) receptor, inhibits platelet aggregation and promotes vasodilatation in pulmonary vascular beds. AFP 07 is a 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki = 0.561 nM).{7236} AFP 07 shows weaker affinity for EP receptors, with Ki values of > 100 nM for EP1-3 and > 10 nM for EP4.{7236} In piglet and rabbit saphenous veins, which express both IP and EP4, the EP4 antagonist AH 23848 reduces AFP 07-mediated relaxation, suggesting that AFP 07 activates EP4 as well as IP, particularly when both receptors are present.{15488}  

     

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  • Prostaglandin I2 is an unstable prostanoid which, through the ‘I prostanoid’ (IP) receptor, inhibits platelet aggregation and promotes vasodilatation in pulmonary vascular beds. AFP 07 is a 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki = 0.561 nM).{7236} AFP 07 shows weaker affinity for EP receptors, with Ki values of > 100 nM for EP1-3 and > 10 nM for EP4.{7236} In piglet and rabbit saphenous veins, which express both IP and EP4, the EP4 antagonist AH 23848 reduces AFP 07-mediated relaxation, suggesting that AFP 07 activates EP4 as well as IP, particularly when both receptors are present.{15488}  

     

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  • Aftin-4 is an inducer of amyloid-β (1-42) (Aβ42).{45169} It selectively increases extracellular Aβ42 over Aβ40 production in N2a-AβPP695 cells when used at concentrations ranging from 1 to 100 mM. In vivo, aftin-4 (3-20 nmol/animal, i.c.v.) increases hippocampal Aβ42 content, lipid peroxidation, and production of the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in mice.{45170} It also induces spatial working and spatial reference memory deficits in mice, effects that are reversed by co-administration of the γ-secretase inhibitor BMS-299,897.  

     

    Brand:
    Cayman
    SKU:27341 - 1 mg

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  • Aftin-4 is an inducer of amyloid-β (1-42) (Aβ42).{45169} It selectively increases extracellular Aβ42 over Aβ40 production in N2a-AβPP695 cells when used at concentrations ranging from 1 to 100 mM. In vivo, aftin-4 (3-20 nmol/animal, i.c.v.) increases hippocampal Aβ42 content, lipid peroxidation, and production of the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in mice.{45170} It also induces spatial working and spatial reference memory deficits in mice, effects that are reversed by co-administration of the γ-secretase inhibitor BMS-299,897.  

     

    Brand:
    Cayman
    SKU:27341 - 10 mg

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  • Aftin-4 is an inducer of amyloid-β (1-42) (Aβ42).{45169} It selectively increases extracellular Aβ42 over Aβ40 production in N2a-AβPP695 cells when used at concentrations ranging from 1 to 100 mM. In vivo, aftin-4 (3-20 nmol/animal, i.c.v.) increases hippocampal Aβ42 content, lipid peroxidation, and production of the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in mice.{45170} It also induces spatial working and spatial reference memory deficits in mice, effects that are reversed by co-administration of the γ-secretase inhibitor BMS-299,897.  

     

    Brand:
    Cayman
    SKU:27341 - 25 mg

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  • Aftin-4 is an inducer of amyloid-β (1-42) (Aβ42).{45169} It selectively increases extracellular Aβ42 over Aβ40 production in N2a-AβPP695 cells when used at concentrations ranging from 1 to 100 mM. In vivo, aftin-4 (3-20 nmol/animal, i.c.v.) increases hippocampal Aβ42 content, lipid peroxidation, and production of the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in mice.{45170} It also induces spatial working and spatial reference memory deficits in mice, effects that are reversed by co-administration of the γ-secretase inhibitor BMS-299,897.  

     

    Brand:
    Cayman
    SKU:27341 - 5 mg

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  • Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.{30969} It preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies with minimal effect on glucose homeostasis.{30969} Afuresertib demonstrates activity against multiple myeloma in both preclinical and clinical models.{30969,30970}  

     

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  • Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.{30969} It preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies with minimal effect on glucose homeostasis.{30969} Afuresertib demonstrates activity against multiple myeloma in both preclinical and clinical models.{30969,30970}  

     

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  • Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.{30969} It preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies with minimal effect on glucose homeostasis.{30969} Afuresertib demonstrates activity against multiple myeloma in both preclinical and clinical models.{30969,30970}  

     

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    Cayman
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  • Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.{30969} It preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies with minimal effect on glucose homeostasis.{30969} Afuresertib demonstrates activity against multiple myeloma in both preclinical and clinical models.{30969,30970}  

     

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  • Afzelin is a polyphenolic glycoside flavone that has been found in B. pinnatum and has diverse biological activities.{21664,57170,57171} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 6.44 μg/ml.{21664} Afzelin is active against S. aureus, P. aeruginosa, S. typhi, C. albicans, C. parapsilosis, and C. neoformans (MICs = 8, 16, 2, 16, 4, and 4 μg/ml, respectively). It inhibits the proliferation of A549, SKOV3, and SK-MEL-2 cells (EC50s = 40.6, 34.5, and 33.9 μg/ml, respectively).{57170} Afzelin (26 mg/kg per day) reduces the number of eosinophils, other inflammatory cells, and total cells, as well as the levels of IL-4, IL-5, and IL-13, in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma.{57171}  

     

    Brand:
    Cayman
    SKU:31135 - 1 mg

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  • Afzelin is a polyphenolic glycoside flavone that has been found in B. pinnatum and has diverse biological activities.{21664,57170,57171} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 6.44 μg/ml.{21664} Afzelin is active against S. aureus, P. aeruginosa, S. typhi, C. albicans, C. parapsilosis, and C. neoformans (MICs = 8, 16, 2, 16, 4, and 4 μg/ml, respectively). It inhibits the proliferation of A549, SKOV3, and SK-MEL-2 cells (EC50s = 40.6, 34.5, and 33.9 μg/ml, respectively).{57170} Afzelin (26 mg/kg per day) reduces the number of eosinophils, other inflammatory cells, and total cells, as well as the levels of IL-4, IL-5, and IL-13, in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma.{57171}  

     

    Brand:
    Cayman
    SKU:31135 - 10 mg

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  • Afzelin is a polyphenolic glycoside flavone that has been found in B. pinnatum and has diverse biological activities.{21664,57170,57171} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 6.44 μg/ml.{21664} Afzelin is active against S. aureus, P. aeruginosa, S. typhi, C. albicans, C. parapsilosis, and C. neoformans (MICs = 8, 16, 2, 16, 4, and 4 μg/ml, respectively). It inhibits the proliferation of A549, SKOV3, and SK-MEL-2 cells (EC50s = 40.6, 34.5, and 33.9 μg/ml, respectively).{57170} Afzelin (26 mg/kg per day) reduces the number of eosinophils, other inflammatory cells, and total cells, as well as the levels of IL-4, IL-5, and IL-13, in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma.{57171}  

     

    Brand:
    Cayman
    SKU:31135 - 25 mg

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  • Afzelin is a polyphenolic glycoside flavone that has been found in B. pinnatum and has diverse biological activities.{21664,57170,57171} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 6.44 μg/ml.{21664} Afzelin is active against S. aureus, P. aeruginosa, S. typhi, C. albicans, C. parapsilosis, and C. neoformans (MICs = 8, 16, 2, 16, 4, and 4 μg/ml, respectively). It inhibits the proliferation of A549, SKOV3, and SK-MEL-2 cells (EC50s = 40.6, 34.5, and 33.9 μg/ml, respectively).{57170} Afzelin (26 mg/kg per day) reduces the number of eosinophils, other inflammatory cells, and total cells, as well as the levels of IL-4, IL-5, and IL-13, in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma.{57171}  

     

    Brand:
    Cayman
    SKU:31135 - 5 mg

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  • The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK2) receptors to regulate cell proliferation, differentiation, apoptosis, and gene expression of gastrointestinal cells and exerts trophic effects on a number of gastric cancer cell lines. AG-041R is a potent gastrin/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.{16543} AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC50 = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells.{16543,16568} AG-041R (1 µM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered in combination with the selective COX-2 inhibitor NS-398 (Item No. 70590) at 10 µM.{16544}  

     

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    Cayman
    SKU:10010129 - 1 mg

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  • The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK2) receptors to regulate cell proliferation, differentiation, apoptosis, and gene expression of gastrointestinal cells and exerts trophic effects on a number of gastric cancer cell lines. AG-041R is a potent gastrin/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.{16543} AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC50 = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells.{16543,16568} AG-041R (1 µM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered in combination with the selective COX-2 inhibitor NS-398 (Item No. 70590) at 10 µM.{16544}  

     

    Brand:
    Cayman
    SKU:10010129 - 10 mg

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  • The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK2) receptors to regulate cell proliferation, differentiation, apoptosis, and gene expression of gastrointestinal cells and exerts trophic effects on a number of gastric cancer cell lines. AG-041R is a potent gastrin/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.{16543} AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC50 = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells.{16543,16568} AG-041R (1 µM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered in combination with the selective COX-2 inhibitor NS-398 (Item No. 70590) at 10 µM.{16544}  

     

    Brand:
    Cayman
    SKU:10010129 - 5 mg

    Available on backorder

  • The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK2) receptors to regulate cell proliferation, differentiation, apoptosis, and gene expression of gastrointestinal cells and exerts trophic effects on a number of gastric cancer cell lines. AG-041R is a potent gastrin/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.{16543} AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC50 = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells.{16543,16568} AG-041R (1 µM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered in combination with the selective COX-2 inhibitor NS-398 (Item No. 70590) at 10 µM.{16544}  

     

    Brand:
    Cayman
    SKU:10010129 - 50 mg

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  • The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC50 values of 0.4 and 7 μM, respectively.{23639} At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 μM.{23640,23641}  

     

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  • The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC50 values of 0.4 and 7 μM, respectively.{23639} At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 μM.{23640,23641}  

     

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    Cayman
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  • The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC50 values of 0.4 and 7 μM, respectively.{23639} At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 μM.{23640,23641}  

     

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  • AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) that specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of 2-hydroxyglutarate.{32361} AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.{32361}  

     

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    Cayman
    SKU:19894 -

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  • AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) that specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of 2-hydroxyglutarate.{32361} AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.{32361}  

     

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    Cayman
    SKU:19894 -

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  • AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) that specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of 2-hydroxyglutarate.{32361} AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.{32361}  

     

    Brand:
    Cayman
    SKU:19894 -

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  • AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) that specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of 2-hydroxyglutarate.{32361} AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.{32361}  

     

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    Cayman
    SKU:19894 -

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  • Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.{17267,17268} It blocks the production of TNF-α in vitro{17268} and in vivo,{17267} attenuating signaling through NF-κB,{17267} the induced expression of COX-2 and iNOS,{17269,17266} and the inflammatory response in diverse animal models.{17269,17270} AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM){14963} and platelet-derived GFRK (IC50 > 100 μM).{14964}  

     

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    Cayman
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  • Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.{17267,17268} It blocks the production of TNF-α in vitro{17268} and in vivo,{17267} attenuating signaling through NF-κB,{17267} the induced expression of COX-2 and iNOS,{17269,17266} and the inflammatory response in diverse animal models.{17269,17270} AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM){14963} and platelet-derived GFRK (IC50 > 100 μM).{14964}  

     

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    Cayman
    SKU:-
  • Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.{17267,17268} It blocks the production of TNF-α in vitro{17268} and in vivo,{17267} attenuating signaling through NF-κB,{17267} the induced expression of COX-2 and iNOS,{17269,17266} and the inflammatory response in diverse animal models.{17269,17270} AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM){14963} and platelet-derived GFRK (IC50 > 100 μM).{14964}  

     

    Brand:
    Cayman
    SKU:-
  • Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.{17267,17268} It blocks the production of TNF-α in vitro{17268} and in vivo,{17267} attenuating signaling through NF-κB,{17267} the induced expression of COX-2 and iNOS,{17269,17266} and the inflammatory response in diverse animal models.{17269,17270} AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM){14963} and platelet-derived GFRK (IC50 > 100 μM).{14964}  

     

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    Cayman
    SKU:-
  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM).{15594} It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 µM without affecting activity of the EGF receptor.{15594}  

     

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    Cayman
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  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM).{15594} It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 µM without affecting activity of the EGF receptor.{15594}  

     

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    Cayman
    SKU:-
  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM).{15594} It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 µM without affecting activity of the EGF receptor.{15594}  

     

    Brand:
    Cayman
    SKU:-
  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM).{15594} It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 µM without affecting activity of the EGF receptor.{15594}  

     

    Brand:
    Cayman
    SKU:-
  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).{15594} It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. {15594} Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.{15594}  

     

    Brand:
    Cayman
    SKU:10010592 - 1 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).{15594} It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. {15594} Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.{15594}  

     

    Brand:
    Cayman
    SKU:10010592 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).{15594} It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. {15594} Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.{15594}  

     

    Brand:
    Cayman
    SKU:10010592 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.{15153} AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).{15594} It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. {15594} Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.{15594}  

     

    Brand:
    Cayman
    SKU:10010592 - 5 mg

    Available on backorder

  • AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24677 - 1 mg

    Available on backorder

  • AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24677 - 10 mg

    Available on backorder

  • AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24677 - 25 mg

    Available on backorder

  • AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:24677 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block EGFR-dependent cell proliferation. AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.{15153} Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.{15592} AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively.{15593} This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.{15591}  

     

    Brand:
    Cayman
    SKU:10010244 - 1 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block EGFR-dependent cell proliferation. AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.{15153} Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.{15592} AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively.{15593} This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.{15591}  

     

    Brand:
    Cayman
    SKU:10010244 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block EGFR-dependent cell proliferation. AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.{15153} Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.{15592} AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively.{15593} This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.{15591}  

     

    Brand:
    Cayman
    SKU:10010244 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block EGFR-dependent cell proliferation. AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.{15153} Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.{15592} AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively.{15593} This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.{15591}  

     

    Brand:
    Cayman
    SKU:10010244 - 5 mg

    Available on backorder

  • AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194.{32831}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194.{32831}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194.{32831}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194.{32831}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010248 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010248 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010248 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010248 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010300 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010300 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010300 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010300 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 0.8 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010315 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 0.8 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010315 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 0.8 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010315 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 0.8 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010315 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010314 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010314 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010314 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010314 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues.{14963} AG-370 is a selective inhibitor of PDGF receptor kinase with an IC50 value of 20 µM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC50 = 820 µM).{16600,850,16601}  

     

    Brand:
    Cayman
    SKU:10010568 - 1 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues.{14963} AG-370 is a selective inhibitor of PDGF receptor kinase with an IC50 value of 20 µM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC50 = 820 µM).{16600,850,16601}  

     

    Brand:
    Cayman
    SKU:10010568 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues.{14963} AG-370 is a selective inhibitor of PDGF receptor kinase with an IC50 value of 20 µM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC50 = 820 µM).{16600,850,16601}  

     

    Brand:
    Cayman
    SKU:10010568 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues.{14963} AG-370 is a selective inhibitor of PDGF receptor kinase with an IC50 value of 20 µM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC50 = 820 µM).{16600,850,16601}  

     

    Brand:
    Cayman
    SKU:10010568 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (Ptk) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of Ptks. Tyrphostins are a class of antiproliferative compounds which act as Ptk blockers.{14963} Leukemic cells from patients in relapse have constitutively activated JAK2 Ptk. AG-490 is an inhibitor of JAK2 activity and selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 almost completely blocks growth of all pre-B acute leukemia (ALL) cells at a concentration of 5 µM.{2158} Furthermore, inhibition of JAK/STAT signaling in satellite cells via AG-490 and the STAT3 inhibitor 5,15-DPP (Item No. 16090) has been used to stimulate muscle regeneration in a model of aging skeletal muscle deterioration.{27730}  

     

    Brand:
    Cayman
    SKU:10010311 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (Ptk) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of Ptks. Tyrphostins are a class of antiproliferative compounds which act as Ptk blockers.{14963} Leukemic cells from patients in relapse have constitutively activated JAK2 Ptk. AG-490 is an inhibitor of JAK2 activity and selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 almost completely blocks growth of all pre-B acute leukemia (ALL) cells at a concentration of 5 µM.{2158} Furthermore, inhibition of JAK/STAT signaling in satellite cells via AG-490 and the STAT3 inhibitor 5,15-DPP (Item No. 16090) has been used to stimulate muscle regeneration in a model of aging skeletal muscle deterioration.{27730}  

     

    Brand:
    Cayman
    SKU:10010311 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (Ptk) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of Ptks. Tyrphostins are a class of antiproliferative compounds which act as Ptk blockers.{14963} Leukemic cells from patients in relapse have constitutively activated JAK2 Ptk. AG-490 is an inhibitor of JAK2 activity and selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 almost completely blocks growth of all pre-B acute leukemia (ALL) cells at a concentration of 5 µM.{2158} Furthermore, inhibition of JAK/STAT signaling in satellite cells via AG-490 and the STAT3 inhibitor 5,15-DPP (Item No. 16090) has been used to stimulate muscle regeneration in a model of aging skeletal muscle deterioration.{27730}  

     

    Brand:
    Cayman
    SKU:10010311 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (Ptk) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of Ptks. Tyrphostins are a class of antiproliferative compounds which act as Ptk blockers.{14963} Leukemic cells from patients in relapse have constitutively activated JAK2 Ptk. AG-490 is an inhibitor of JAK2 activity and selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 almost completely blocks growth of all pre-B acute leukemia (ALL) cells at a concentration of 5 µM.{2158} Furthermore, inhibition of JAK/STAT signaling in satellite cells via AG-490 and the STAT3 inhibitor 5,15-DPP (Item No. 16090) has been used to stimulate muscle regeneration in a model of aging skeletal muscle deterioration.{27730}  

     

    Brand:
    Cayman
    SKU:10010311 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.{14964}  

     

    Brand:
    Cayman
    SKU:10010242 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.{14964}  

     

    Brand:
    Cayman
    SKU:10010242 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.{14964}  

     

    Brand:
    Cayman
    SKU:10010242 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.{14964}  

     

    Brand:
    Cayman
    SKU:10010242 - 50 mg

    Available on backorder

  • AG-528 is a tyrphostin that inhibits EGFR and HER2 (IC50s = 12 and 4.9 μM, respectively, for inhibition of autophosphorylation).{45071} It also inhibits pantothenate kinase 3 (PanK3; IC50 = 3 μM).{46757} AG-528 inhibits EGF-dependent proliferation of HER14 cells (IC50 = 25 μM).{45071}  

     

    Brand:
    Cayman
    SKU:29666 - 10 mg

    Available on backorder

  • AG-528 is a tyrphostin that inhibits EGFR and HER2 (IC50s = 12 and 4.9 μM, respectively, for inhibition of autophosphorylation).{45071} It also inhibits pantothenate kinase 3 (PanK3; IC50 = 3 μM).{46757} AG-528 inhibits EGF-dependent proliferation of HER14 cells (IC50 = 25 μM).{45071}  

     

    Brand:
    Cayman
    SKU:29666 - 100 mg

    Available on backorder

  • AG-528 is a tyrphostin that inhibits EGFR and HER2 (IC50s = 12 and 4.9 μM, respectively, for inhibition of autophosphorylation).{45071} It also inhibits pantothenate kinase 3 (PanK3; IC50 = 3 μM).{46757} AG-528 inhibits EGF-dependent proliferation of HER14 cells (IC50 = 25 μM).{45071}  

     

    Brand:
    Cayman
    SKU:29666 - 250 mg

    Available on backorder

  • AG-528 is a tyrphostin that inhibits EGFR and HER2 (IC50s = 12 and 4.9 μM, respectively, for inhibition of autophosphorylation).{45071} It also inhibits pantothenate kinase 3 (PanK3; IC50 = 3 μM).{46757} AG-528 inhibits EGF-dependent proliferation of HER14 cells (IC50 = 25 μM).{45071}  

     

    Brand:
    Cayman
    SKU:29666 - 50 mg

    Available on backorder

  • AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM).{45071} It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM.{45071,45072} It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM).{45073}  

     

    Brand:
    Cayman
    SKU:23247 - 10 mg

    Available on backorder

  • AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM).{45071} It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM.{45071,45072} It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM).{45073}  

     

    Brand:
    Cayman
    SKU:23247 - 25 mg

    Available on backorder

  • AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM).{45071} It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM.{45071,45072} It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM).{45073}  

     

    Brand:
    Cayman
    SKU:23247 - 5 mg

    Available on backorder

  • AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM).{45071} It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM.{45071,45072} It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM).{45073}  

     

    Brand:
    Cayman
    SKU:23247 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-82 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 3 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010312 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-82 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 3 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010312 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-82 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 3 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010312 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-82 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 3 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010312 - 50 mg

    Available on backorder

  • The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}  

     

    Brand:
    Cayman
    SKU:10010243 - 1 mg

    Available on backorder

  • The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}  

     

    Brand:
    Cayman
    SKU:10010243 - 10 mg

    Available on backorder

  • The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}  

     

    Brand:
    Cayman
    SKU:10010243 - 5 mg

    Available on backorder

  • The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}  

     

    Brand:
    Cayman
    SKU:10010243 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.{14963} AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).{15153} Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.{19455} AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.{19454}  

     

    Brand:
    Cayman
    SKU:10793 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.{14963} AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).{15153} Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.{19455} AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.{19454}  

     

    Brand:
    Cayman
    SKU:10793 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.{14963} AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).{15153} Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.{19455} AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.{19454}  

     

    Brand:
    Cayman
    SKU:10793 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.{14963} AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).{15153} Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.{19455} AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.{19454}  

     

    Brand:
    Cayman
    SKU:10793 - 50 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010313 - 10 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010313 - 25 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010313 - 5 mg

    Available on backorder

  • Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation.{14963} AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.{14963}  

     

    Brand:
    Cayman
    SKU:10010313 - 50 mg

    Available on backorder

  • Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases.{15153} AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 µM, respectively, for human proteins).{29184} It also inhibits epidermal growth factor receptor (IC50 = 0.25 µM).{29184} As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line.{29187,29186} AG957 is also used to study signaling through c-Abl.{29185}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases.{15153} AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 µM, respectively, for human proteins).{29184} It also inhibits epidermal growth factor receptor (IC50 = 0.25 µM).{29184} As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line.{29187,29186} AG957 is also used to study signaling through c-Abl.{29185}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases.{15153} AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 µM, respectively, for human proteins).{29184} It also inhibits epidermal growth factor receptor (IC50 = 0.25 µM).{29184} As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line.{29187,29186} AG957 is also used to study signaling through c-Abl.{29185}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Agarotetrol is a chromone derivative originally isolated from agarwood, a component of incense and traditional medicines.{53078,53079}  

     

    Brand:
    Cayman
    SKU:27662 - 1 mg

    Available on backorder

  • Agarotetrol is a chromone derivative originally isolated from agarwood, a component of incense and traditional medicines.{53078,53079}  

     

    Brand:
    Cayman
    SKU:27662 - 10 mg

    Available on backorder

  • Agarotetrol is a chromone derivative originally isolated from agarwood, a component of incense and traditional medicines.{53078,53079}  

     

    Brand:
    Cayman
    SKU:27662 - 25 mg

    Available on backorder

  • Agarotetrol is a chromone derivative originally isolated from agarwood, a component of incense and traditional medicines.{53078,53079}  

     

    Brand:
    Cayman
    SKU:27662 - 5 mg

    Available on backorder

  • Glycolaldehyde-pyridine (GA-pyridine) is an advanced glycation end product (AGE).{15062,49055} It is formed via the reaction of GA, a product of myeloperoxidase activity, with lysine and can therefore serve as an antigenic marker of protein modification resulting from myeloperoxidase activity.{15062} GA-pyridine has been detected in the tubular epithelial cells, renal vasculature, and glomerular epithelium of both healthy and diseased human kidneys, and accumulates in the glomerular mesangium of patients with renal diseases, including diabetic nephropathy, Wegener’s granulomatosis, mesangial proliferative glomerulonephritis, and focal glomerular sclerosis.{49055} GA-pyridine also accumulates in the cytoplasm of foam cells and extracellularly in the atheromatous core of human atherosclerotic lesions.{15062} Cayman’s AGE (GA-Pyridine Specific) Monoclonal Antibody (Clone 1F10) can be used for Western blot and ELISA applications. This antibody recognizes GA AGE-modified proteins.  

     

    Brand:
    Cayman
    SKU:27271 - 100 µg

    Available on backorder

  • Immunogen: GA-pyridine-BSA • Host: Mouse • Cross Reactivity: (-) (Carboxyethyl)-lysine (CEL), Glyoxal (GO), Methyl-glyoxal (MG) • Species reactivity: (+) Human • Applications: WB, ELISA  

     

    Brand:
    Cayman
    SKU:27271- 100 µg

    Available on backorder

  • Immunogen: GA-pyridine-BSA • Host: Mouse • Cross Reactivity: (-) (Carboxyethyl)-lysine (CEL), Glyoxal (GO), Methyl-glyoxal (MG) • Species reactivity: (+) Human • Applications: WB, ELISA  

     

    Brand:
    Cayman
    SKU:27271- 100 µg
  • Glycolaldehyde-pyridine (GA-pyridine) is an advanced glycation end product (AGE).{15062,49055} It is formed via the reaction of GA, a product of myeloperoxidase activity, with lysine and can therefore serve as an antigenic marker of protein modification resulting from myeloperoxidase activity.{15062} GA-pyridine has been detected in the tubular epithelial cells, renal vasculature, and glomerular epithelium of both healthy and diseased human kidneys, and accumulates in the glomerular mesangium of patients with renal diseases, including diabetic nephropathy, Wegener’s granulomatosis, mesangial proliferative glomerulonephritis, and focal glomerular sclerosis.{49055} GA-pyridine also accumulates in the cytoplasm of foam cells and extracellularly in the atheromatous core of human atherosclerotic lesions.{15062} Cayman’s AGE (GA-Pyridine Specific) Monoclonal Antibody (Clone 3G2) can be used for Western blot and ELISA applications. This antibody recognizes GA AGE-modified proteins.  

     

    Brand:
    Cayman
    SKU:27272 - 100 µg

    Available on backorder

  • Immunogen: GA-pyridine-BSA • Host: Mouse • Cross Reactivity: (-) (Carboxyethyl)-lysine (CEL), Glyoxal (GO), Methyl-glyoxal (MG) • Applications: WB, ELISA  

     

    Brand:
    Cayman
    SKU:27272- 100 µg

    Available on backorder

  • Immunogen: GA-pyridine-BSA • Host: Mouse • Cross Reactivity: (-) (Carboxyethyl)-lysine (CEL), Glyoxal (GO), Methyl-glyoxal (MG) • Applications: WB, ELISA  

     

    Brand:
    Cayman
    SKU:27272- 100 µg
  • Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing a-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-5198 is a potent, selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively, but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM).{23141} AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2‑HG production in HT1080 and U87MG cells with IC50 values of 0.48 and 0.07 µM, respectively.{23140} In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts.{23141} Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.{23141}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing a-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-5198 is a potent, selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively, but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM).{23141} AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2‑HG production in HT1080 and U87MG cells with IC50 values of 0.48 and 0.07 µM, respectively.{23140} In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts.{23141} Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.{23141}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing a-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-5198 is a potent, selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively, but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM).{23141} AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2‑HG production in HT1080 and U87MG cells with IC50 values of 0.48 and 0.07 µM, respectively.{23140} In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts.{23141} Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.{23141}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing a-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-5198 is a potent, selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively, but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM).{23141} AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2‑HG production in HT1080 and U87MG cells with IC50 values of 0.48 and 0.07 µM, respectively.{23140} In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts.{23141} Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.{23141}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.{23425} It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.{23425} In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.{23245}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.{23425} It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.{23425} In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.{23245}  

     

    Brand:
    Cayman
    SKU:-
  • Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.{23425} It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.{23425} In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.{23245}  

     

    Brand:
    Cayman
    SKU:-
  • Agistatin B is a fungal metabolite originally isolated from Fusarium.{49004}  

     

    Brand:
    Cayman
    SKU:26600 - 1 mg

    Available on backorder

  • Agistatin B is a fungal metabolite originally isolated from Fusarium.{49004}  

     

    Brand:
    Cayman
    SKU:26600 - 5 mg

    Available on backorder

  • Agistatin D is a pyranacetal fungal metabolite that has been found in the soil fungus FH-A 6239.{49004}  

     

    Brand:
    Cayman
    SKU:29169 - 1 mg

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  • Agistatin E is a fungal metabolite originally isolated from Fusarium.{47752}  

     

    Brand:
    Cayman
    SKU:29211 - 1 mg

    Available on backorder

  • Agistatin E is a fungal metabolite originally isolated from Fusarium.{47752}  

     

    Brand:
    Cayman
    SKU:29211 - 500 µg

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  • Mammalian sirtuin 2 (SIRT2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) with roles in cell cycle progression and tumorigenesis. AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495} It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression.{17495} AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.  

     

    Brand:
    Cayman
    SKU:-
  • Mammalian sirtuin 2 (SIRT2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) with roles in cell cycle progression and tumorigenesis. AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495} It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression.{17495} AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.  

     

    Brand:
    Cayman
    SKU:-
  • Mammalian sirtuin 2 (SIRT2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) with roles in cell cycle progression and tumorigenesis. AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495} It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression.{17495} AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.  

     

    Brand:
    Cayman
    SKU:-
  • Mammalian sirtuin 2 (SIRT2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) with roles in cell cycle progression and tumorigenesis. AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495} It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression.{17495} AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.  

     

    Brand:
    Cayman
    SKU:-
  • AGK2 (Item No. 13145) is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495,16624} AGK7 is an inactive control to be used in experiments with AGK2. It differs from AGK2, structurally, only in the position of nitrogen in the quinoline group.{17495} AGK7 has IC50 values greater than 50 µM on SIRT1 and SIRT2 and greater than 5 µM on SIRT3.{17495}  

     

    Brand:
    Cayman
    SKU:-
  • AGK2 (Item No. 13145) is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495,16624} AGK7 is an inactive control to be used in experiments with AGK2. It differs from AGK2, structurally, only in the position of nitrogen in the quinoline group.{17495} AGK7 has IC50 values greater than 50 µM on SIRT1 and SIRT2 and greater than 5 µM on SIRT3.{17495}  

     

    Brand:
    Cayman
    SKU:-
  • AGK2 (Item No. 13145) is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495,16624} AGK7 is an inactive control to be used in experiments with AGK2. It differs from AGK2, structurally, only in the position of nitrogen in the quinoline group.{17495} AGK7 has IC50 values greater than 50 µM on SIRT1 and SIRT2 and greater than 5 µM on SIRT3.{17495}  

     

    Brand:
    Cayman
    SKU:-
  • AGK2 (Item No. 13145) is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.{17495,16624} AGK7 is an inactive control to be used in experiments with AGK2. It differs from AGK2, structurally, only in the position of nitrogen in the quinoline group.{17495} AGK7 has IC50 values greater than 50 µM on SIRT1 and SIRT2 and greater than 5 µM on SIRT3.{17495}  

     

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    Cayman
    SKU:-
  • AGL 2263 is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R; IC50 = 0.43 μM).{25699} It also inhibits the insulin receptor (IR), protein kinase B (PKB), and Src in a cell-free assay (IC50s = 0.4, 55, and 2.2 μM, respectively). AGL 2263 inhibits IGF-1R autophosphorylation and phosphorylation of the downstream elements IRS-1, PKB, and ERK2 in an ATP-independent manner. It inhibits colony formation of PC3 and LNCaP prostate and MCF-7 and MDA-MB-468 breast cancer cells in soft agar (IC50s = 4.3, 9, 17, and 6 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21776 -

    Out of stock

  • AGL 2263 is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R; IC50 = 0.43 μM).{25699} It also inhibits the insulin receptor (IR), protein kinase B (PKB), and Src in a cell-free assay (IC50s = 0.4, 55, and 2.2 μM, respectively). AGL 2263 inhibits IGF-1R autophosphorylation and phosphorylation of the downstream elements IRS-1, PKB, and ERK2 in an ATP-independent manner. It inhibits colony formation of PC3 and LNCaP prostate and MCF-7 and MDA-MB-468 breast cancer cells in soft agar (IC50s = 4.3, 9, 17, and 6 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21776 -

    Out of stock

  • AGL 2263 is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R; IC50 = 0.43 μM).{25699} It also inhibits the insulin receptor (IR), protein kinase B (PKB), and Src in a cell-free assay (IC50s = 0.4, 55, and 2.2 μM, respectively). AGL 2263 inhibits IGF-1R autophosphorylation and phosphorylation of the downstream elements IRS-1, PKB, and ERK2 in an ATP-independent manner. It inhibits colony formation of PC3 and LNCaP prostate and MCF-7 and MDA-MB-468 breast cancer cells in soft agar (IC50s = 4.3, 9, 17, and 6 μM, respectively).  

     

    Brand:
    Cayman
    SKU:21776 -

    Out of stock

  • Agmatine is a metabolite formed during polyamine biosynthesis with diverse biological activities.{37373} Agmatine is released from and taken up by synaptosomes, demonstrating neurotransmitter-like activity. It binds to human adrenergic receptors (ARs) and imidazoline (I) receptors (Kis = 46.98, 164.4, 26.3, and 74.4 μM for α2A-, α2B-, and α2c-ARs and I2b, respectively).{37374} Agmatine acts as an antagonist of the NMDA receptor (NMDAR) in a voltage- and concentration-dependent manner in primary rat hippocampal neurons and antagonizes nicotinic acetylcholine receptors (nAChRs) in intact chick retina at 1 mM.{37375},{37376} It is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 in mouse N1E-115 neuroblastoma cells (IC50 = 141 μM) and blocks ATP-sensitive potassium channels (KATP) in a concentration-dependent manner in mouse islets of Langerhans β-cells.{37377},{37378} Agmatine competitively inhibits neuronal, macrophage, endothelial, and inducible nitric oxide synthase (NOS; Kis = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (Ki = 29 μM).{37379} In vivo, agmatine (10 mg/kg) lowers the ED50 value by 5.2- and 4.7-fold for morphine (Item No. ISO60147) and [D-Pen2,D-Pen5]enkephalin (DPDPE), respectively, in mice in a tail flick assay.{37380} It increases the nephron filtration rate when microperfused into the urinary space of rats, an effect that is reversed by the non-selective NOS inhibitor L-NG-monomethyl arginine (L-NMMA; Item Nos. 80200, 10005031).{37381}  

     

    Brand:
    Cayman
    SKU:23513 - 1 g

    Available on backorder

  • Agmatine is a metabolite formed during polyamine biosynthesis with diverse biological activities.{37373} Agmatine is released from and taken up by synaptosomes, demonstrating neurotransmitter-like activity. It binds to human adrenergic receptors (ARs) and imidazoline (I) receptors (Kis = 46.98, 164.4, 26.3, and 74.4 μM for α2A-, α2B-, and α2c-ARs and I2b, respectively).{37374} Agmatine acts as an antagonist of the NMDA receptor (NMDAR) in a voltage- and concentration-dependent manner in primary rat hippocampal neurons and antagonizes nicotinic acetylcholine receptors (nAChRs) in intact chick retina at 1 mM.{37375},{37376} It is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 in mouse N1E-115 neuroblastoma cells (IC50 = 141 μM) and blocks ATP-sensitive potassium channels (KATP) in a concentration-dependent manner in mouse islets of Langerhans β-cells.{37377},{37378} Agmatine competitively inhibits neuronal, macrophage, endothelial, and inducible nitric oxide synthase (NOS; Kis = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (Ki = 29 μM).{37379} In vivo, agmatine (10 mg/kg) lowers the ED50 value by 5.2- and 4.7-fold for morphine (Item No. ISO60147) and [D-Pen2,D-Pen5]enkephalin (DPDPE), respectively, in mice in a tail flick assay.{37380} It increases the nephron filtration rate when microperfused into the urinary space of rats, an effect that is reversed by the non-selective NOS inhibitor L-NG-monomethyl arginine (L-NMMA; Item Nos. 80200, 10005031).{37381}  

     

    Brand:
    Cayman
    SKU:23513 - 10 g

    Available on backorder

  • Agmatine is a metabolite formed during polyamine biosynthesis with diverse biological activities.{37373} Agmatine is released from and taken up by synaptosomes, demonstrating neurotransmitter-like activity. It binds to human adrenergic receptors (ARs) and imidazoline (I) receptors (Kis = 46.98, 164.4, 26.3, and 74.4 μM for α2A-, α2B-, and α2c-ARs and I2b, respectively).{37374} Agmatine acts as an antagonist of the NMDA receptor (NMDAR) in a voltage- and concentration-dependent manner in primary rat hippocampal neurons and antagonizes nicotinic acetylcholine receptors (nAChRs) in intact chick retina at 1 mM.{37375},{37376} It is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 in mouse N1E-115 neuroblastoma cells (IC50 = 141 μM) and blocks ATP-sensitive potassium channels (KATP) in a concentration-dependent manner in mouse islets of Langerhans β-cells.{37377},{37378} Agmatine competitively inhibits neuronal, macrophage, endothelial, and inducible nitric oxide synthase (NOS; Kis = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (Ki = 29 μM).{37379} In vivo, agmatine (10 mg/kg) lowers the ED50 value by 5.2- and 4.7-fold for morphine (Item No. ISO60147) and [D-Pen2,D-Pen5]enkephalin (DPDPE), respectively, in mice in a tail flick assay.{37380} It increases the nephron filtration rate when microperfused into the urinary space of rats, an effect that is reversed by the non-selective NOS inhibitor L-NG-monomethyl arginine (L-NMMA; Item Nos. 80200, 10005031).{37381}  

     

    Brand:
    Cayman
    SKU:23513 - 5 g

    Available on backorder

  • AGN 193109-d7 is intended for use as an internal standard for the quantification of AGN 193109 (Item No. 23975) by GC- or LC-MS. AGN 193109 is an antagonist of retinoic acid receptors (RARs).{41300} AGN 193109 decreases expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, markers of retinoid action in ECE16-1 cells, when co-administered with TTNPB (Item No. 16144) but not when used alone. In vivo, AGN 193109 induces cleft palate or frontonasal dysplasia and eye malformations in fetuses of pregnant mice following a single oral dose of 1 mg/kg.{41301}     

     

    Brand:
    Cayman
    SKU:23976 - 1 mg

    Available on backorder

  • Agnuside is an iridoid glycoside originally isolated from V. rotundifolia fruit that has diverse biological activities.{42077,42078,42079,42080} It inhibits COX-2 with an IC50 value of 0.026 mg/ml but exhibits less than 10% inhibition of COX-1 at this concentration.{42077} It also inhibits 46.3, 66.8, and 82.1% of P-glycoprotein (P-gp) ATPase activity at concentrations of 5, 25, and 100 μM, respectively.{25373} Agnuside (0.1-10 μM) induces proliferation of MCF-7 breast cancer cells, an effect that is inhibited by the estrogen receptor antagonist fulvestrant (ICI 182780; Item No. 10011269).{42078} In vivo, agnuside (50 mg/kg) reduces acetic acid-induced writhing in mice indicating analgesia.{42079} It also suppresses production of the pro-inflammatory mediators prostaglandin E2 (PGE2) and leukotriene B4 (LTB4; Item No. 20110) and the T cell-mediated cytokines IL-2, TNF-α, INF-γ, IL-4, IL-10, and IL-17 in splenocytes and arthritic paw tissue from arthritic adrenalectomized rats.{42080}  

     

    Brand:
    Cayman
    SKU:24971 - 1 mg

    Available on backorder

  • Agnuside is an iridoid glycoside originally isolated from V. rotundifolia fruit that has diverse biological activities.{42077,42078,42079,42080} It inhibits COX-2 with an IC50 value of 0.026 mg/ml but exhibits less than 10% inhibition of COX-1 at this concentration.{42077} It also inhibits 46.3, 66.8, and 82.1% of P-glycoprotein (P-gp) ATPase activity at concentrations of 5, 25, and 100 μM, respectively.{25373} Agnuside (0.1-10 μM) induces proliferation of MCF-7 breast cancer cells, an effect that is inhibited by the estrogen receptor antagonist fulvestrant (ICI 182780; Item No. 10011269).{42078} In vivo, agnuside (50 mg/kg) reduces acetic acid-induced writhing in mice indicating analgesia.{42079} It also suppresses production of the pro-inflammatory mediators prostaglandin E2 (PGE2) and leukotriene B4 (LTB4; Item No. 20110) and the T cell-mediated cytokines IL-2, TNF-α, INF-γ, IL-4, IL-10, and IL-17 in splenocytes and arthritic paw tissue from arthritic adrenalectomized rats.{42080}  

     

    Brand:
    Cayman
    SKU:24971 - 10 mg

    Available on backorder

  • Agnuside is an iridoid glycoside originally isolated from V. rotundifolia fruit that has diverse biological activities.{42077,42078,42079,42080} It inhibits COX-2 with an IC50 value of 0.026 mg/ml but exhibits less than 10% inhibition of COX-1 at this concentration.{42077} It also inhibits 46.3, 66.8, and 82.1% of P-glycoprotein (P-gp) ATPase activity at concentrations of 5, 25, and 100 μM, respectively.{25373} Agnuside (0.1-10 μM) induces proliferation of MCF-7 breast cancer cells, an effect that is inhibited by the estrogen receptor antagonist fulvestrant (ICI 182780; Item No. 10011269).{42078} In vivo, agnuside (50 mg/kg) reduces acetic acid-induced writhing in mice indicating analgesia.{42079} It also suppresses production of the pro-inflammatory mediators prostaglandin E2 (PGE2) and leukotriene B4 (LTB4; Item No. 20110) and the T cell-mediated cytokines IL-2, TNF-α, INF-γ, IL-4, IL-10, and IL-17 in splenocytes and arthritic paw tissue from arthritic adrenalectomized rats.{42080}  

     

    Brand:
    Cayman
    SKU:24971 - 25 mg

    Available on backorder