Cayman
Showing 10801–10950 of 45550 results
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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:CaymanSKU:10011336 - 500 µgAvailable 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:CaymanSKU:28059 - 5 mgAvailable 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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:28051 - 1 mgAvailable 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:CaymanSKU:28051 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-Available on backorder
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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:29135 - 10 mgAvailable 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:CaymanSKU:29135 - 25 mgAvailable 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:CaymanSKU:29135 - 5 mgAvailable 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:CaymanSKU:29135 - 50 mgAvailable on backorder
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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:-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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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:CaymanSKU:28079 - 1 mgAvailable 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:CaymanSKU:28079 - 10 mgAvailable 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:CaymanSKU:28079 - 25 mgAvailable 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:CaymanSKU:28079 - 5 mgAvailable 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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:23836 - 10 gAvailable 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:CaymanSKU:23836 - 100 gAvailable 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:CaymanSKU:23836 - 25 gAvailable 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:CaymanSKU:23836 - 5 gAvailable 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:CaymanSKU:30198 - 1 mgAvailable 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:CaymanSKU:30198 - 10 mgAvailable 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:CaymanSKU:30198 - 25 mgAvailable 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:CaymanSKU:30198 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:27333 - 1 mgAvailable 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:CaymanSKU:27333 - 10 mgAvailable 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:CaymanSKU:27333 - 25 mgAvailable 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:CaymanSKU:27333 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:28042 - 1 mgAvailable 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:CaymanSKU:28042 - 5 mgAvailable 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:CaymanSKU:26676 - 1 mgAvailable 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:CaymanSKU:26676 - 500 µgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:29460 - 1 mgAvailable 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:CaymanSKU:29460 - 10 mgAvailable 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:CaymanSKU:29460 - 25 mgAvailable 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:CaymanSKU:29460 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:25444 - 1 mgAvailable 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:CaymanSKU:25444 - 10 mgAvailable 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:CaymanSKU:25444 - 25 mgAvailable 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:CaymanSKU:25444 - 5 mgAvailable 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:CaymanSKU:-Available on backorder