Cayman
Showing 44401–44550 of 45550 results
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Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.{24477} WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.{24478,24477} At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.{24477} Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.{24477}
Brand:CaymanSKU:- Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.{24477} WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.{24478,24477} At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.{24477} Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.{24477}
Brand:CaymanSKU:- Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.{24477} WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.{24478,24477} At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.{24477} Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.{24477}
Brand:CaymanSKU:-
WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway.{32144} It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a model of retinal degeneration.{32669}
Brand:CaymanSKU:-Available on backorder
WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway.{32144} It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a model of retinal degeneration.{32669}
Brand:CaymanSKU:-Available on backorder
WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway.{32144} It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a model of retinal degeneration.{32669}
Brand:CaymanSKU:-Available on backorder
WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway.{32144} It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a model of retinal degeneration.{32669}
Brand:CaymanSKU:-Available on backorder
WS6 is a compound that stimulates the proliferation of pancreatic β cells in rodent and human primary islets (ECmax = 200 and 400 nM, respectively, over four days).{32144,32143} It promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation.{32144} WS6 also stimulates α cell proliferation in human pancreatic islets.{32142} WS6 appears to act by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription.{32144}
Brand:CaymanSKU:-Available on backorder
WS6 is a compound that stimulates the proliferation of pancreatic β cells in rodent and human primary islets (ECmax = 200 and 400 nM, respectively, over four days).{32144,32143} It promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation.{32144} WS6 also stimulates α cell proliferation in human pancreatic islets.{32142} WS6 appears to act by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription.{32144}
Brand:CaymanSKU:-Available on backorder
WS6 is a compound that stimulates the proliferation of pancreatic β cells in rodent and human primary islets (ECmax = 200 and 400 nM, respectively, over four days).{32144,32143} It promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation.{32144} WS6 also stimulates α cell proliferation in human pancreatic islets.{32142} WS6 appears to act by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription.{32144}
Brand:CaymanSKU:-Available on backorder
WS6 is a compound that stimulates the proliferation of pancreatic β cells in rodent and human primary islets (ECmax = 200 and 400 nM, respectively, over four days).{32144,32143} It promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation.{32144} WS6 also stimulates α cell proliferation in human pancreatic islets.{32142} WS6 appears to act by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription.{32144}
Brand:CaymanSKU:-Available on backorder
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-1 is a reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells. Through a reaction-based fluorescent turn-on strategy, WSP-1 selectively and rapidly reacts with H2S to generate benzodithiolone and a fluorophore with excitation and emission maxima of 465 and 515 nm, respectively.{20172}
Brand:CaymanSKU:11179 - 1 mgAvailable on backorder
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-1 is a reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells. Through a reaction-based fluorescent turn-on strategy, WSP-1 selectively and rapidly reacts with H2S to generate benzodithiolone and a fluorophore with excitation and emission maxima of 465 and 515 nm, respectively.{20172}
Brand:CaymanSKU:11179 - 10 mgAvailable on backorder
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-1 is a reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells. Through a reaction-based fluorescent turn-on strategy, WSP-1 selectively and rapidly reacts with H2S to generate benzodithiolone and a fluorophore with excitation and emission maxima of 465 and 515 nm, respectively.{20172}
Brand:CaymanSKU:11179 - 5 mgAvailable on backorder
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-5 is a turn-on fluorescent probe for hydrogen sulfide (H2S).{27272} Upon reaction with H2S, WSP-5 releases a fluorophore that displays excitation/emission maxima of 502/525 nm, respectively. WSP-5 exhibits a faster turn-on rate and a more sensitive detection limit toward H2S than WSP-1 (Item No. 11179).
Brand:CaymanSKU:-Out of stock
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-5 is a turn-on fluorescent probe for hydrogen sulfide (H2S).{27272} Upon reaction with H2S, WSP-5 releases a fluorophore that displays excitation/emission maxima of 502/525 nm, respectively. WSP-5 exhibits a faster turn-on rate and a more sensitive detection limit toward H2S than WSP-1 (Item No. 11179).
Brand:CaymanSKU:-Out of stock
Hydrogen sulfide (H2S) is an important gaseous mediator, like nitric oxide, that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. WSP-5 is a turn-on fluorescent probe for hydrogen sulfide (H2S).{27272} Upon reaction with H2S, WSP-5 releases a fluorophore that displays excitation/emission maxima of 502/525 nm, respectively. WSP-5 exhibits a faster turn-on rate and a more sensitive detection limit toward H2S than WSP-1 (Item No. 11179).
Brand:CaymanSKU:-Out of stock
Defining the mechanisms responsible for alterations in cell cycle progression is crucial to understanding many human diseases, most notably cancer. Cell proliferation assays have been widely used to assess cell cycle regulatory factors such as growth factors, cytokines, mitogens, and drugs.{14191} Cayman’s WST-1 Proliferation Assay Kit provides an easy to use tool for studying the induction and inhibition of cell proliferation in any in vitro model. The assay is based on the reduction of tetrazolium salt WST-1 to soluble formazan by electron transport across the plasma membrane of dividing cells. This kit will also allow investigators to screen drug candidates involved in regulation of cell cycle.
Brand:CaymanSKU:10008883 - 480 wellsAvailable on backorder
Defining the mechanisms responsible for alterations in cell cycle progression is crucial to understanding many human diseases, most notably cancer. Cell proliferation assays have been widely used to assess cell cycle regulatory factors such as growth factors, cytokines, mitogens, and drugs.{14191} Cayman’s WST-1 Proliferation Assay Kit provides an easy to use tool for studying the induction and inhibition of cell proliferation in any in vitro model. The assay is based on the reduction of tetrazolium salt WST-1 to soluble formazan by electron transport across the plasma membrane of dividing cells. This kit will also allow investigators to screen drug candidates involved in regulation of cell cycle.
Brand:CaymanSKU:10008883 - 96 wellsAvailable on backorder
WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity. At neutral pH and in the presence of the intermediate electron acceptor, 1-methoxy phenazine methosulfate, NADPH-dependent cellular oxidoreductases, acting via plasma membrane electron transport, reduce the cell-impermeant WST-8 outside the cell to a water-soluble formazan dye with absorbance max at 460 nm.{10833,30333} It is typically used as a cell viability indicator in cell proliferation assays.
Brand:CaymanSKU:-Available on backorder
WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity. At neutral pH and in the presence of the intermediate electron acceptor, 1-methoxy phenazine methosulfate, NADPH-dependent cellular oxidoreductases, acting via plasma membrane electron transport, reduce the cell-impermeant WST-8 outside the cell to a water-soluble formazan dye with absorbance max at 460 nm.{10833,30333} It is typically used as a cell viability indicator in cell proliferation assays.
Brand:CaymanSKU:-Available on backorder
WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity. At neutral pH and in the presence of the intermediate electron acceptor, 1-methoxy phenazine methosulfate, NADPH-dependent cellular oxidoreductases, acting via plasma membrane electron transport, reduce the cell-impermeant WST-8 outside the cell to a water-soluble formazan dye with absorbance max at 460 nm.{10833,30333} It is typically used as a cell viability indicator in cell proliferation assays.
Brand:CaymanSKU:-Available on backorder
WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity. At neutral pH and in the presence of the intermediate electron acceptor, 1-methoxy phenazine methosulfate, NADPH-dependent cellular oxidoreductases, acting via plasma membrane electron transport, reduce the cell-impermeant WST-8 outside the cell to a water-soluble formazan dye with absorbance max at 460 nm.{10833,30333} It is typically used as a cell viability indicator in cell proliferation assays.
Brand:CaymanSKU:-Available on backorder
Cayman’s WST-8 Cell Proliferation Assay provides a tool for studying induction and inhibition of cell proliferation in any in vitro model. The assay is based on the extracellular reduction of WST-8 by NADH produced in the mitochondria resulting in a water-soluble formazan which dissolves directly into the culture medium. Cayman’s WST-8 assay is preferred when higher cell densities are expected, as up to 5 x 106 cells/ml can be successfully quantified.
Brand:CaymanSKU:10010199 - 480 wellsAvailable on backorder
Cayman’s WST-8 Cell Proliferation Assay provides a tool for studying induction and inhibition of cell proliferation in any in vitro model. The assay is based on the extracellular reduction of WST-8 by NADH produced in the mitochondria resulting in a water-soluble formazan which dissolves directly into the culture medium. Cayman’s WST-8 assay is preferred when higher cell densities are expected, as up to 5 x 106 cells/ml can be successfully quantified.
Brand:CaymanSKU:10010199 - 96 wellsAvailable on backorder
WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.
Brand:CaymanSKU:21099 -Out of stock
WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.
Brand:CaymanSKU:21099 -Out of stock
WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.
Brand:CaymanSKU:21099 -Out of stock
WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.
Brand:CaymanSKU:21099 -Out of stock
Mouse carboxylesterase 3 (Ces3, also named Ces 1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL113 is a selective inhibitor of Ces3 and the structurally related Ces 1f (IC50 = ~0.1 µM) without significantly affecting several related enzymes.{26463} It significantly reduces basal lipolysis in adipocytes.{26463} More interestingly, WWL113 corrects multiple features of metabolic syndrome in obese-diabetic db/db mice, including changes in weight gain, glucose tolerance, and levels of nonesterified free fatty acids, triglycerides, total cholesterol, and fasted glucose.{26463} It has similar effects in mice with diet-induced obesity.{26463} WWL113 also inhibits the human ortholog of mouse Ces3, hCES1 (IC50 = ~50 nM), which has a similar tissue expression pattern to Ces3.{26464,26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces 1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL113 is a selective inhibitor of Ces3 and the structurally related Ces 1f (IC50 = ~0.1 µM) without significantly affecting several related enzymes.{26463} It significantly reduces basal lipolysis in adipocytes.{26463} More interestingly, WWL113 corrects multiple features of metabolic syndrome in obese-diabetic db/db mice, including changes in weight gain, glucose tolerance, and levels of nonesterified free fatty acids, triglycerides, total cholesterol, and fasted glucose.{26463} It has similar effects in mice with diet-induced obesity.{26463} WWL113 also inhibits the human ortholog of mouse Ces3, hCES1 (IC50 = ~50 nM), which has a similar tissue expression pattern to Ces3.{26464,26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces 1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL113 is a selective inhibitor of Ces3 and the structurally related Ces 1f (IC50 = ~0.1 µM) without significantly affecting several related enzymes.{26463} It significantly reduces basal lipolysis in adipocytes.{26463} More interestingly, WWL113 corrects multiple features of metabolic syndrome in obese-diabetic db/db mice, including changes in weight gain, glucose tolerance, and levels of nonesterified free fatty acids, triglycerides, total cholesterol, and fasted glucose.{26463} It has similar effects in mice with diet-induced obesity.{26463} WWL113 also inhibits the human ortholog of mouse Ces3, hCES1 (IC50 = ~50 nM), which has a similar tissue expression pattern to Ces3.{26464,26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces 1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL113 is a selective inhibitor of Ces3 and the structurally related Ces 1f (IC50 = ~0.1 µM) without significantly affecting several related enzymes.{26463} It significantly reduces basal lipolysis in adipocytes.{26463} More interestingly, WWL113 corrects multiple features of metabolic syndrome in obese-diabetic db/db mice, including changes in weight gain, glucose tolerance, and levels of nonesterified free fatty acids, triglycerides, total cholesterol, and fasted glucose.{26463} It has similar effects in mice with diet-induced obesity.{26463} WWL113 also inhibits the human ortholog of mouse Ces3, hCES1 (IC50 = ~50 nM), which has a similar tissue expression pattern to Ces3.{26464,26463}
Brand:CaymanSKU:-
The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (Item No. 62160) to regulate its availability at cannabinoid receptors.{15253} WWL123 is a brain-penetrant inhibitor of ABHD6 (IC50 = 0.43 µM) that demonstrates >10-fold selectivity for ABHD6 compared to a panel of ~35 other serine hydrolases.{27126} Inhibition of ABHD6 by WWL123 has been used to decrease seizure incidence in a genetic mouse model of juvenile Huntington’s disease as well as in chemically-induced epilepsy models.{27125}
Brand:CaymanSKU:-Out of stock
The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (Item No. 62160) to regulate its availability at cannabinoid receptors.{15253} WWL123 is a brain-penetrant inhibitor of ABHD6 (IC50 = 0.43 µM) that demonstrates >10-fold selectivity for ABHD6 compared to a panel of ~35 other serine hydrolases.{27126} Inhibition of ABHD6 by WWL123 has been used to decrease seizure incidence in a genetic mouse model of juvenile Huntington’s disease as well as in chemically-induced epilepsy models.{27125}
Brand:CaymanSKU:-Out of stock
The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (Item No. 62160) to regulate its availability at cannabinoid receptors.{15253} WWL123 is a brain-penetrant inhibitor of ABHD6 (IC50 = 0.43 µM) that demonstrates >10-fold selectivity for ABHD6 compared to a panel of ~35 other serine hydrolases.{27126} Inhibition of ABHD6 by WWL123 has been used to decrease seizure incidence in a genetic mouse model of juvenile Huntington’s disease as well as in chemically-induced epilepsy models.{27125}
Brand:CaymanSKU:-Out of stock
The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (Item No. 62160) to regulate its availability at cannabinoid receptors.{15253} WWL123 is a brain-penetrant inhibitor of ABHD6 (IC50 = 0.43 µM) that demonstrates >10-fold selectivity for ABHD6 compared to a panel of ~35 other serine hydrolases.{27126} Inhibition of ABHD6 by WWL123 has been used to decrease seizure incidence in a genetic mouse model of juvenile Huntington’s disease as well as in chemically-induced epilepsy models.{27125}
Brand:CaymanSKU:-Out of stock
Mouse carboxylesterase 3 (Ces3, also named Ces1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL229 is a selective inhibitor of Ces3 (IC50 = 1.94 µM) that has no significant effect on other, related enzymes.{26463} By inhibiting the triglyceride hydrolase activity of Ces3, WWL229 promotes lipid storage in cultured adipocytes and prevents basal lipolysis.{26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL229 is a selective inhibitor of Ces3 (IC50 = 1.94 µM) that has no significant effect on other, related enzymes.{26463} By inhibiting the triglyceride hydrolase activity of Ces3, WWL229 promotes lipid storage in cultured adipocytes and prevents basal lipolysis.{26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL229 is a selective inhibitor of Ces3 (IC50 = 1.94 µM) that has no significant effect on other, related enzymes.{26463} By inhibiting the triglyceride hydrolase activity of Ces3, WWL229 promotes lipid storage in cultured adipocytes and prevents basal lipolysis.{26463}
Brand:CaymanSKU:- Mouse carboxylesterase 3 (Ces3, also named Ces1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL229 is a selective inhibitor of Ces3 (IC50 = 1.94 µM) that has no significant effect on other, related enzymes.{26463} By inhibiting the triglyceride hydrolase activity of Ces3, WWL229 promotes lipid storage in cultured adipocytes and prevents basal lipolysis.{26463}
Brand:CaymanSKU:-
WWL70 is an inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 70 nM).{15297} It increases the expression of the adipose browning-related gene Ucp1 in differentiated 3T3-L1 mouse adipocytes and increases the oxygen consumption rate (OCR), an effect that can be blocked by the PPARα antagonist GW 6471 (Item No. 11697), when used at a concentration of 10 µM.{53349} WWL70 (10 mg/kg per day) also increases the expression of the adipose browning-related genes Ucp1, Prdm16, Tmem26, and Tbx1 in visceral adipose tissue in mice fed a high-fat diet. WWL70 reduces adipose tissue mass and prevents glucose-intolerance and increases in body weight in mice fed a high-fat diet but does not reduce hepatic triacylglycerol levels.{53350} It increases brain levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) and decreases the severity of experimental autoimmune encephalomyelitis (EAE) in wild-type, but not cannabinoid (CB) receptor 2 (CB2) knockout, mice when administered at a dose of 10 mg/kg per day starting at disease onset.{53351}
Brand:CaymanSKU:10011213 - 1 mgAvailable on backorder
WWL70 is an inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 70 nM).{15297} It increases the expression of the adipose browning-related gene Ucp1 in differentiated 3T3-L1 mouse adipocytes and increases the oxygen consumption rate (OCR), an effect that can be blocked by the PPARα antagonist GW 6471 (Item No. 11697), when used at a concentration of 10 µM.{53349} WWL70 (10 mg/kg per day) also increases the expression of the adipose browning-related genes Ucp1, Prdm16, Tmem26, and Tbx1 in visceral adipose tissue in mice fed a high-fat diet. WWL70 reduces adipose tissue mass and prevents glucose-intolerance and increases in body weight in mice fed a high-fat diet but does not reduce hepatic triacylglycerol levels.{53350} It increases brain levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) and decreases the severity of experimental autoimmune encephalomyelitis (EAE) in wild-type, but not cannabinoid (CB) receptor 2 (CB2) knockout, mice when administered at a dose of 10 mg/kg per day starting at disease onset.{53351}
Brand:CaymanSKU:10011213 - 10 mgAvailable on backorder
WWL70 is an inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 70 nM).{15297} It increases the expression of the adipose browning-related gene Ucp1 in differentiated 3T3-L1 mouse adipocytes and increases the oxygen consumption rate (OCR), an effect that can be blocked by the PPARα antagonist GW 6471 (Item No. 11697), when used at a concentration of 10 µM.{53349} WWL70 (10 mg/kg per day) also increases the expression of the adipose browning-related genes Ucp1, Prdm16, Tmem26, and Tbx1 in visceral adipose tissue in mice fed a high-fat diet. WWL70 reduces adipose tissue mass and prevents glucose-intolerance and increases in body weight in mice fed a high-fat diet but does not reduce hepatic triacylglycerol levels.{53350} It increases brain levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) and decreases the severity of experimental autoimmune encephalomyelitis (EAE) in wild-type, but not cannabinoid (CB) receptor 2 (CB2) knockout, mice when administered at a dose of 10 mg/kg per day starting at disease onset.{53351}
Brand:CaymanSKU:10011213 - 25 mgAvailable on backorder
WWL70 is an inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 70 nM).{15297} It increases the expression of the adipose browning-related gene Ucp1 in differentiated 3T3-L1 mouse adipocytes and increases the oxygen consumption rate (OCR), an effect that can be blocked by the PPARα antagonist GW 6471 (Item No. 11697), when used at a concentration of 10 µM.{53349} WWL70 (10 mg/kg per day) also increases the expression of the adipose browning-related genes Ucp1, Prdm16, Tmem26, and Tbx1 in visceral adipose tissue in mice fed a high-fat diet. WWL70 reduces adipose tissue mass and prevents glucose-intolerance and increases in body weight in mice fed a high-fat diet but does not reduce hepatic triacylglycerol levels.{53350} It increases brain levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) and decreases the severity of experimental autoimmune encephalomyelitis (EAE) in wild-type, but not cannabinoid (CB) receptor 2 (CB2) knockout, mice when administered at a dose of 10 mg/kg per day starting at disease onset.{53351}
Brand:CaymanSKU:10011213 - 5 mgAvailable on backorder
Wy 14643 is a peroxisome proliferator-activated receptor (PPAR activator). Although this compound is primarily an activator of PPARα,{3458,6573,6549} it activates PPARγ as well.{4044} Activation of PPARδ by Wy 14643 is also observed,{6161} but this finding is rare. The potency of Wy 14643 as an activator of PPARα is species dependent, with receptor activation occurring at concentrations as low as 0.1 µM in the mouse compared to 10 µM in Xenopus.{5592}
Brand:CaymanSKU:70730 - 10 mgAvailable on backorder
Wy 14643 is a peroxisome proliferator-activated receptor (PPAR activator). Although this compound is primarily an activator of PPARα,{3458,6573,6549} it activates PPARγ as well.{4044} Activation of PPARδ by Wy 14643 is also observed,{6161} but this finding is rare. The potency of Wy 14643 as an activator of PPARα is species dependent, with receptor activation occurring at concentrations as low as 0.1 µM in the mouse compared to 10 µM in Xenopus.{5592}
Brand:CaymanSKU:70730 - 250 mgAvailable on backorder
Wy 14643 is a peroxisome proliferator-activated receptor (PPAR activator). Although this compound is primarily an activator of PPARα,{3458,6573,6549} it activates PPARγ as well.{4044} Activation of PPARδ by Wy 14643 is also observed,{6161} but this finding is rare. The potency of Wy 14643 as an activator of PPARα is species dependent, with receptor activation occurring at concentrations as low as 0.1 µM in the mouse compared to 10 µM in Xenopus.{5592}
Brand:CaymanSKU:70730 - 5 mgAvailable on backorder
Wy 14643 is a peroxisome proliferator-activated receptor (PPAR activator). Although this compound is primarily an activator of PPARα,{3458,6573,6549} it activates PPARγ as well.{4044} Activation of PPARδ by Wy 14643 is also observed,{6161} but this finding is rare. The potency of Wy 14643 as an activator of PPARα is species dependent, with receptor activation occurring at concentrations as low as 0.1 µM in the mouse compared to 10 µM in Xenopus.{5592}
Brand:CaymanSKU:70730 - 50 mgAvailable on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.{29888} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.{29888} WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.{29888} Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.{29888} In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.{29887}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.{29888} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.{29888} WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.{29888} Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.{29888} In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.{29887}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.{29888} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.{29888} WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.{29888} Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.{29888} In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.{29887}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.{29888} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.{29888} WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.{29888} Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.{29888} In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.{29887}
Brand:CaymanSKU:-Available on backorder
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.45 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 661 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = 42 nM).
Brand:CaymanSKU:21199 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.45 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 661 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = 42 nM).
Brand:CaymanSKU:21199 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.45 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 661 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = 42 nM).
Brand:CaymanSKU:21199 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.45 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 661 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = 42 nM).
Brand:CaymanSKU:21199 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.08 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 6 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = <1 nM).
Brand:CaymanSKU:21200 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.08 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 6 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = <1 nM).
Brand:CaymanSKU:21200 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.08 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 6 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = <1 nM).
Brand:CaymanSKU:21200 -Out of stock
WYE-23 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.08 nM).{20314,48484} It is selective for mTOR over PI3Kα (IC50 = 6 nM).{20314} WYE-23 inhibits cell growth in LNCaP cells (IC50 = <1 nM).
Brand:CaymanSKU:21200 -Out of stock
WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.{17537,20134} It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.{20314} WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.{17537}
Brand:CaymanSKU:- WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.{17537,20134} It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.{20314} WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.{17537}
Brand:CaymanSKU:- WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.{17537,20134} It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.{20314} WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.{17537}
Brand:CaymanSKU:- WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.{17537,20134} It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.{20314} WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.{17537}
Brand:CaymanSKU:-
WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).{17537} It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.{53480}
Brand:CaymanSKU:29977 - 1 mgAvailable on backorder
WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).{17537} It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.{53480}
Brand:CaymanSKU:29977 - 10 mgAvailable on backorder
WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).{17537} It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.{53480}
Brand:CaymanSKU:29977 - 25 mgAvailable on backorder
WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).{17537} It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.{53480}
Brand:CaymanSKU:29977 - 5 mgAvailable on backorder
WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).{41787}
Brand:CaymanSKU:23440 - 1 mgAvailable on backorder
WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).{41787}
Brand:CaymanSKU:23440 - 10 mgAvailable on backorder
WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).{41787}
Brand:CaymanSKU:23440 - 5 mgAvailable on backorder
WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).{41787}
Brand:CaymanSKU:23440 - 50 mgAvailable on backorder
The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.{27827,27829} WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC50 = 8 nM).{27829,27826} It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.{27829} WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.{27829} Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.{27825,27822,27824,27823}
Brand:CaymanSKU:-Out of stock
The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.{27827,27829} WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC50 = 8 nM).{27829,27826} It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.{27829} WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.{27829} Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.{27825,27822,27824,27823}
Brand:CaymanSKU:-Out of stock
The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.{27827,27829} WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC50 = 8 nM).{27829,27826} It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.{27829} WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.{27829} Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.{27825,27822,27824,27823}
Brand:CaymanSKU:-Out of stock
The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.{27827,27829} WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC50 = 8 nM).{27829,27826} It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.{27829} WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.{27829} Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.{27825,27822,27824,27823}
Brand:CaymanSKU:-Out of stock
NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. WZ4003 is a selective inhibitor of NUAK1 and NUAK2 (IC50s = 20 and 100 nM, respectively).{30771} It does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.{30771} At 3-10 µM, WZ4003 has been shown to inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.{30771} When administered to mouse embryonic fibroblasts in vitro, 10 µM WZ4003 inhibits proliferation and migration in a wound-healing assay.{30771} It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.{30771}
Brand:CaymanSKU:-Available on backorder
NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. WZ4003 is a selective inhibitor of NUAK1 and NUAK2 (IC50s = 20 and 100 nM, respectively).{30771} It does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.{30771} At 3-10 µM, WZ4003 has been shown to inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.{30771} When administered to mouse embryonic fibroblasts in vitro, 10 µM WZ4003 inhibits proliferation and migration in a wound-healing assay.{30771} It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.{30771}
Brand:CaymanSKU:-Available on backorder
NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. WZ4003 is a selective inhibitor of NUAK1 and NUAK2 (IC50s = 20 and 100 nM, respectively).{30771} It does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.{30771} At 3-10 µM, WZ4003 has been shown to inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.{30771} When administered to mouse embryonic fibroblasts in vitro, 10 µM WZ4003 inhibits proliferation and migration in a wound-healing assay.{30771} It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.{30771}
Brand:CaymanSKU:-Available on backorder
NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. WZ4003 is a selective inhibitor of NUAK1 and NUAK2 (IC50s = 20 and 100 nM, respectively).{30771} It does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.{30771} At 3-10 µM, WZ4003 has been shown to inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.{30771} When administered to mouse embryonic fibroblasts in vitro, 10 µM WZ4003 inhibits proliferation and migration in a wound-healing assay.{30771} It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.{30771}
Brand:CaymanSKU:-Available on backorder