Cayman

Showing 10801–10950 of 45550 results

  • Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).{15451} Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells. {15451}  

     

    Brand:
    Cayman
    SKU:10011336 - 500 µg

    Available on backorder

  • Averantin is an anthraquinone fungal metabolite that has been found in Aspergillus.{48478,48479} It is an intermediate in the biosynthesis of aflatoxin B1 (Item No. 11293).{48478} Averantin is active against B. subtilis bacteria and the plant pathogenic fungus F. solani in vitro (MICs = 16-32 μg/ml).{48479}  

     

    Brand:
    Cayman
    SKU:28059 - 5 mg

    Available on backorder

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABAA receptor.{35015,35017,35019} Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel.{35019} Avermectin B1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (Kis = 1.3 and 3.6 µM, respectively).{35020} Formulations containing avermectin B1a (>80%) and avermectin B1b (~20%; Item No. 17453) are used in insecticides and veterinary anthelmintic formulas as abamectin (Item No. 19201).{35016,35018}  

     

    Brand:
    Cayman
    SKU:22000 -

    Out of stock

  • Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a (Item No. 22000).{46109} It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.{35146}  

     

    Brand:
    Cayman
    SKU:28051 - 1 mg

    Available on backorder

  • Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a (Item No. 22000).{46109} It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.{35146}  

     

    Brand:
    Cayman
    SKU:28051 - 5 mg

    Available on backorder

  • Avermectins are insecticides and anthelmintics first isolated from broths fermented by S. avermitilis.{28251} They potentiate glutamate- and GABA-gated chloride channel opening in nematodes.{26993,28250} Avermectin B1b is a minor component of avermectin broth.{26993} Avermectins, including avermectin B1b, are used broadly against nematodes, ticks, flies, and ants.{26993}  

     

    Brand:
    Cayman
    SKU:-

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  • Avermectins are insecticides and anthelmintics first isolated from broths fermented by S. avermitilis.{28251} They potentiate glutamate- and GABA-gated chloride channel opening in nematodes.{26993,28250} Avermectin B1b is a minor component of avermectin broth.{26993} Avermectins, including avermectin B1b, are used broadly against nematodes, ticks, flies, and ants.{26993}  

     

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    Cayman
    SKU:-

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  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avibactam is a β-lactamase inhibitor (IC50s = 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively).{39116,39113} It restores the antimicrobial activity of ceftazidime (Item No. 14828), ceftriaxone (Item No. 18866), imipenem (Item No. 16039), and piperacillin (Item No. 20766) against antibiotic-resistant Enterobacteriaceae in vitro (MIC90 reduction 4-1,024-fold across 190 E. coli and K. pneumoniae clinical isolates).{39114} Formulations containing avibactam have been used to treat carbapenem-resistant Enterobacteriaceae infections.{39115}  

     

    Brand:
    Cayman
    SKU:22825 -

    Out of stock

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 10 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 25 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 5 mg

    Available on backorder

  • Avilamycin A is an antibiotic.{45579} It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).{45579,45580} Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.{45581} Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock.  

     

    Brand:
    Cayman
    SKU:29135 - 50 mg

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  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR.{33610} In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.{33610}  

     

    Brand:
    Cayman
    SKU:21387 -

    Out of stock

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

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  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

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  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.{30733,30731} AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.{30731,30732} In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).{30731,30642,30732}  

     

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    Cayman
    SKU:-

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 1 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 10 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 25 mg

    Available on backorder

  • AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).{52052} It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.  

     

    Brand:
    Cayman
    SKU:28079 - 5 mg

    Available on backorder

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • AVN944 is a selective, noncompetitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH; Ki = 6-10 nM for both human IMPDH isoforms), a rate-limiting enzyme involved in the de novo synthesis of purine nucleotides.{33492} Inhibition of IMPDH results in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 has been shown to inhibit the proliferation of multiple myeloma cells in vitro by inducing caspase-independent apoptosis.{33492} It is also reported to have antitumor properties in androgen-sensitive and androgen-independent prostate cancer cells in vitro.{33491}  

     

    Brand:
    Cayman
    SKU:21284 -

    Out of stock

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 10 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 100 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 25 g

    Available on backorder

  • Avobenzone is a full-spectrum ultraviolet A (UVA) blocker.{41451} It inhibits UVA-induced melanin and tyrosinase activity in B16/F10 melanoma cells (IC30s = 21.94 and 24.25 μM, respectively).{41452} Avobenzone (30 μM) also inhibits UVA-induced production of reactive oxygen species (ROS) and 8-hydroxy-2′-deoxyguanosine (8-OH-dG; Item No. 89320) and depletion of glutathione (GSH; Item No. 10007461) in B16/F10 cells. It increases nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and upregulates the antioxidant response element (ARE) in UVA-irradiated B16/F10 cells at a concentration of 30 μM. Formulations containing avobenzone have been used as a sun protectant in sunscreen products.  

     

    Brand:
    Cayman
    SKU:23836 - 5 g

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 1 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 10 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 25 mg

    Available on backorder

  • Avridine is a synthetic lipid amine that acts as an adjuvant.{48943} Subplantar injection of avridine induces paw swelling, an effect that can be blocked by the non-steroidal anti-inflammatory drug (NSAID) phenylbutazone (Item No. 70400) or the alkylating agent cyclophosphamide (Item No. 13849), in rats. Avridine induces paw joint tissue destruction, bone and pannus formation, and neutrophil, fibroblast, and osteoclast infiltration in the same model. It also increases the number of CD4+ T and MHC class II+ cells in rat paws when administered at a dose of 1.5 mg/animal.{48944} Avridine has been used to induce experimental rheumatoid arthritis in rats.{48944,48945,48946}  

     

    Brand:
    Cayman
    SKU:30198 - 5 mg

    Available on backorder

  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.{29595} This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).{29595} AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.{29593,29594,29596} It has a superior pharmacokinetic profile in dogs vs. humans.{29594,29592}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.{1474} AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.{18000} At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.{18000}  

     

    Brand:
    Cayman
    SKU:-
  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 1 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 10 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 25 mg

    Available on backorder

  • AX-024 is an inhibitor of the CD3ε-Nck interaction.{49065} It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).  

     

    Brand:
    Cayman
    SKU:27333 - 5 mg

    Available on backorder

  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:-
  • Axitinib sulfoxide is a major inactive metabolite of the tyrosine kinase inhibitor axitinib (Item No. 13813).{43878,43879} It is formed from axitinib primarily by the cytochrome P450 (CYP) isoform CYP3A4 with minor contributions from CYP3A5 and CYP2C19.{43878}  

     

    Brand:
    Cayman
    SKU:28042 - 1 mg

    Available on backorder

  • Axitinib sulfoxide is a major inactive metabolite of the tyrosine kinase inhibitor axitinib (Item No. 13813).{43878,43879} It is formed from axitinib primarily by the cytochrome P450 (CYP) isoform CYP3A4 with minor contributions from CYP3A5 and CYP2C19.{43878}  

     

    Brand:
    Cayman
    SKU:28042 - 5 mg

    Available on backorder

  • Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib (Item No. 13813) by GC- or LC-MS. Axitinib (Item No. 13813) is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:26676 - 1 mg

    Available on backorder

  • Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib (Item No. 13813) by GC- or LC-MS. Axitinib (Item No. 13813) is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).{18372} It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).{57053} Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.  

     

    Brand:
    Cayman
    SKU:26676 - 500 µg

    Available on backorder

  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AY 9944 prevents cholesterol biosynthesis by inhibiting the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50 = 13 nM), which interferes with the conversion of 7-dehydro cholesterol (Item No. 14612) to cholesterol.{27278,27282} Furthermore, by upregulating the expression of DHCR7, AY 9944 can block Hedgehog signaling at the level of Smoothened or by loss of Suppressor of Fused.{27279} AY 9944 inhibition of DHCR7 has been used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.{27282,27280} However, AY 9944 is highly teratogenic, producing congenital defects in offspring when fed to pregnant animals.{27281}  

     

    Brand:
    Cayman
    SKU:-
  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 1 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 10 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 25 mg

    Available on backorder

  • AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

     

    Brand:
    Cayman
    SKU:29460 - 5 mg

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. AZ 20 is a potent inhibitor of ATR (IC50 = 5 nM).{28669} It displays 7.6-fold selectivity over mTOR and minimal activity against a panel of 442 other kinases, including ataxia telangiectasia mutated. AZ 20 inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro. It is orally bioavailable and significantly reduces the growth of LoVo xenografts in mice.{28669}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 3146 is an inhibitor of the monopolar spindle 1 (Mps1) checkpoint kinase (IC50 = 35 nM).{33103} It displays selectivity over 46 other kinases including Cdk1 and Aurora kinase B.{33103} It has been shown to inhibit the recruitment of Mad1, Mad2, and centromere protein E (CENP-E) to kinetochores.{33103} AZ 3146 can be used with GSK923295 (Item No. 18389), an inhibitor of CENP-E, to generate aneuploidy in cells.{31964}  

     

    Brand:
    Cayman
    SKU:19991 -

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 1 mg

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 10 mg

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 25 mg

    Available on backorder

  • AZ 33 is an inhibitor of lactate dehydrogenase A (LDHA; Kd = 0.093 μM; IC50 = 0.5 μM).{36785} It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).{36786} AZ 33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 = >500 μM).  

     

    Brand:
    Cayman
    SKU:25444 - 5 mg

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50s = 15-17 nM) that spares the wild-type form of the receptor (IC50 = 480 nM).{27820,32544,32545} AZ 5104 displays a similar overall activity profile as the parent compound.{32544,32545}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.{32525} It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).{32525} By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.{32525}  

     

    Brand:
    Cayman
    SKU:19898 -

    Available on backorder

  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

     

    Brand:
    Cayman
    SKU:-
  • AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:29671 - 1 mg

    Available on backorder

  • AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:29671 - 10 mg

    Available on backorder

  • AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:29671 - 25 mg

    Available on backorder

  • AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:29671 - 5 mg

    Available on backorder

  • AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.  

     

    Brand:
    Cayman
    SKU:21898 -

    Out of stock

  • AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.  

     

    Brand:
    Cayman
    SKU:21898 -

    Out of stock

  • AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.  

     

    Brand:
    Cayman
    SKU:21898 -

    Out of stock

  • AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.  

     

    Brand:
    Cayman
    SKU:21898 -

    Out of stock

  • AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).  

     

    Brand:
    Cayman
    SKU:30292 - 1 mg

    Available on backorder

  • AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).  

     

    Brand:
    Cayman
    SKU:30292 - 10 mg

    Available on backorder

  • AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).  

     

    Brand:
    Cayman
    SKU:30292 - 25 mg

    Available on backorder

  • AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).  

     

    Brand:
    Cayman
    SKU:30292 - 5 mg

    Available on backorder

  • Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}  

     

    Brand:
    Cayman
    SKU:27303 - 10 g

    Available on backorder

  • Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}  

     

    Brand:
    Cayman
    SKU:27303 - 100 g

    Available on backorder

  • Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}  

     

    Brand:
    Cayman
    SKU:27303 - 25 g

    Available on backorder

  • Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}  

     

    Brand:
    Cayman
    SKU:27303 - 50 g

    Available on backorder

  • Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}  

     

    Brand:
    Cayman
    SKU:21893 -

    Out of stock

  • Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}  

     

    Brand:
    Cayman
    SKU:21893 -

    Out of stock

  • Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}  

     

    Brand:
    Cayman
    SKU:21893 -

    Out of stock

  • Azadirachtin B is an azadirachtin that has been found in the neem tree, A. indica, and has diverse biological activities, including insecticidal, nematocidal, anticancer, and osteogenic properties.{46667,46668,46669,46670,46671} It has antifeedant activity against P. xylostella third instar larvae when used at a concentration of 3 mg/ml and induces mortality with an LC50 of 1.03 mg/ml.{46668} It induces mortality in M. incognita second instar larvae with an LD50 value of 125.8 ppm.{46669} Azadirachtin B (780 nmol in the drinking water) reduces the number of papillomas formed on mouse skin in a model of skin carcinogenesis induced by peroxynitrite and phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) but is not cytotoxic to HL-60, A549, AZ521, SK-BR-3, or CRL1579 cancer cells (IC50s = >20 µM for all).{46670,46671} It induces osteoblast differentiation and increases the rate of osteoblast proliferation in primary calvarial osteoblast cells when used at concentrations of 100 pM and 10 nM but not 1 pM, 1 µM, or 100 µM.{46667}  

     

    Brand:
    Cayman
    SKU:29569 - 1 mg

    Available on backorder

  • Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}  

     

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    Cayman
    SKU:-
  • Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}  

     

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    Cayman
    SKU:-
  • Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}  

     

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    Cayman
    SKU:-
  • Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}  

     

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    Cayman
    SKU:-
  • Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}  

     

    Brand:
    Cayman
    SKU:28383 - 10 mg

    Available on backorder

  • Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}  

     

    Brand:
    Cayman
    SKU:28383 - 100 mg

    Available on backorder

  • Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}  

     

    Brand:
    Cayman
    SKU:28383 - 25 mg

    Available on backorder

  • Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}  

     

    Brand:
    Cayman
    SKU:28383 - 50 mg

    Available on backorder

  • Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}  

     

    Brand:
    Cayman
    SKU:29758 - 100 mg

    Available on backorder

  • Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}  

     

    Brand:
    Cayman
    SKU:29758 - 250 mg

    Available on backorder

  • Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}  

     

    Brand:
    Cayman
    SKU:29758 - 50 mg

    Available on backorder

  • Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}  

     

    Brand:
    Cayman
    SKU:29758 - 500 mg

    Available on backorder

  • Azathioprine is a purine analog with immunosuppressive effects.{21835} It serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with the proliferation of lymphocytes and other myeloid cells.{21835,21834} Its immunomodulating actions are used to benefit inflammatory bowel disease, as well as a wide range of additional diseases with immunological or autoimmunological components, including rheumatoid arthritis and lupus nephritis.{21835,21834,21833}  

     

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    Cayman
    SKU:-
  • Azathioprine is a purine analog with immunosuppressive effects.{21835} It serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with the proliferation of lymphocytes and other myeloid cells.{21835,21834} Its immunomodulating actions are used to benefit inflammatory bowel disease, as well as a wide range of additional diseases with immunological or autoimmunological components, including rheumatoid arthritis and lupus nephritis.{21835,21834,21833}  

     

    Brand:
    Cayman
    SKU:-
  • AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.  

     

    Brand:
    Cayman
    SKU:25648 - 10 mg

    Available on backorder

  • AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.  

     

    Brand:
    Cayman
    SKU:25648 - 25 mg

    Available on backorder

  • AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.  

     

    Brand:
    Cayman
    SKU:25648 - 5 mg

    Available on backorder

  • AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.  

     

    Brand:
    Cayman
    SKU:25648 - 50 mg

    Available on backorder

  • AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}  

     

    Brand:
    Cayman
    SKU:29827 - 1 mg

    Available on backorder

  • AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}  

     

    Brand:
    Cayman
    SKU:29827 - 10 mg

    Available on backorder

  • AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}  

     

    Brand:
    Cayman
    SKU:29827 - 5 mg

    Available on backorder

  • The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock