Cayman

Showing 32551–32700 of 45550 results

  • NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively.{33325} It synergistically inhibits cell proliferation when used in combination with gefitinib (Item No. 13166) or erlotinib (Item No. 10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors.{33325} NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells.{33326} It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.{33326}  

     

    Brand:
    Cayman
    SKU:19627 -

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  • NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively.{33325} It synergistically inhibits cell proliferation when used in combination with gefitinib (Item No. 13166) or erlotinib (Item No. 10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors.{33325} NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells.{33326} It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.{33326}  

     

    Brand:
    Cayman
    SKU:19627 -

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  • Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.{29237,26276} Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.{29237,26276} NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM).{29235,29236} It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.{29235,29236} Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.{29235}  

     

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    Cayman
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  • Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.{29237,26276} Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.{29237,26276} NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM).{29235,29236} It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.{29235,29236} Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.{29235}  

     

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    Cayman
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  • Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.{29237,26276} Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.{29237,26276} NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM).{29235,29236} It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.{29235,29236} Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.{29235}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.{29237,26276} Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.{29237,26276} NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM).{29235,29236} It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.{29235,29236} Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.{29235}  

     

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    Cayman
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  • Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke.{21993,21995} NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively).{21992} At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes.{21992} At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.{21994}  

     

    Brand:
    Cayman
    SKU:11989 - 10 mg

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  • Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke.{21993,21995} NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively).{21992} At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes.{21992} At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.{21994}  

     

    Brand:
    Cayman
    SKU:11989 - 25 mg

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  • Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke.{21993,21995} NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively).{21992} At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes.{21992} At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.{21994}  

     

    Brand:
    Cayman
    SKU:11989 - 5 mg

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  • NQ301 is a naphthoquinone with diverse biological activities, including antiplatelet, antithrombotic, anti-inflammatory, and antimicrobial properties.{46244,46245,46246,46247} It inhibits rabbit platelet aggregation induced by the thromboxane A2 receptor agonist U-46619 (Item No. 16450) in vitro (IC50 = 0.58 μM) and inhibits the conversion of arachidonic acid to thromboxane B2 in rabbit platelets in a concentration-dependent manner.{46244} It also inhibits human platelet aggregation induced by ADP, collagen, epinephrine, and the calcium ionophore A23187 in vitro (IC50s = 3.21, 15.69, 8.44, and 44.2 μM, respectively).{46245} NQ301 (50 and 100 mg/kg) increases tail bleeding time and exhibits a protective effect against pulmonary thrombosis in mice. It inhibits the protein tyrosine phosphatase CD45 with an IC50 value of 0.29 μM.{46246} NQ301 (3 mg/kg) inhibits ovalbumin-induced footpad swelling in a mouse model of delayed-type hypersensitivity. It is also active against C. albicans, A. niger, B. subtilis, S. aureus, E. coli, and P. aeruginosa (MICs = 12.5-50 μg/ml).{46247}  

     

    Brand:
    Cayman
    SKU:21958 -

    Out of stock

  • NQ301 is a naphthoquinone with diverse biological activities, including antiplatelet, antithrombotic, anti-inflammatory, and antimicrobial properties.{46244,46245,46246,46247} It inhibits rabbit platelet aggregation induced by the thromboxane A2 receptor agonist U-46619 (Item No. 16450) in vitro (IC50 = 0.58 μM) and inhibits the conversion of arachidonic acid to thromboxane B2 in rabbit platelets in a concentration-dependent manner.{46244} It also inhibits human platelet aggregation induced by ADP, collagen, epinephrine, and the calcium ionophore A23187 in vitro (IC50s = 3.21, 15.69, 8.44, and 44.2 μM, respectively).{46245} NQ301 (50 and 100 mg/kg) increases tail bleeding time and exhibits a protective effect against pulmonary thrombosis in mice. It inhibits the protein tyrosine phosphatase CD45 with an IC50 value of 0.29 μM.{46246} NQ301 (3 mg/kg) inhibits ovalbumin-induced footpad swelling in a mouse model of delayed-type hypersensitivity. It is also active against C. albicans, A. niger, B. subtilis, S. aureus, E. coli, and P. aeruginosa (MICs = 12.5-50 μg/ml).{46247}  

     

    Brand:
    Cayman
    SKU:21958 -

    Out of stock

  • NQ301 is a naphthoquinone with diverse biological activities, including antiplatelet, antithrombotic, anti-inflammatory, and antimicrobial properties.{46244,46245,46246,46247} It inhibits rabbit platelet aggregation induced by the thromboxane A2 receptor agonist U-46619 (Item No. 16450) in vitro (IC50 = 0.58 μM) and inhibits the conversion of arachidonic acid to thromboxane B2 in rabbit platelets in a concentration-dependent manner.{46244} It also inhibits human platelet aggregation induced by ADP, collagen, epinephrine, and the calcium ionophore A23187 in vitro (IC50s = 3.21, 15.69, 8.44, and 44.2 μM, respectively).{46245} NQ301 (50 and 100 mg/kg) increases tail bleeding time and exhibits a protective effect against pulmonary thrombosis in mice. It inhibits the protein tyrosine phosphatase CD45 with an IC50 value of 0.29 μM.{46246} NQ301 (3 mg/kg) inhibits ovalbumin-induced footpad swelling in a mouse model of delayed-type hypersensitivity. It is also active against C. albicans, A. niger, B. subtilis, S. aureus, E. coli, and P. aeruginosa (MICs = 12.5-50 μg/ml).{46247}  

     

    Brand:
    Cayman
    SKU:21958 -

    Out of stock

  • NQ301 is a naphthoquinone with diverse biological activities, including antiplatelet, antithrombotic, anti-inflammatory, and antimicrobial properties.{46244,46245,46246,46247} It inhibits rabbit platelet aggregation induced by the thromboxane A2 receptor agonist U-46619 (Item No. 16450) in vitro (IC50 = 0.58 μM) and inhibits the conversion of arachidonic acid to thromboxane B2 in rabbit platelets in a concentration-dependent manner.{46244} It also inhibits human platelet aggregation induced by ADP, collagen, epinephrine, and the calcium ionophore A23187 in vitro (IC50s = 3.21, 15.69, 8.44, and 44.2 μM, respectively).{46245} NQ301 (50 and 100 mg/kg) increases tail bleeding time and exhibits a protective effect against pulmonary thrombosis in mice. It inhibits the protein tyrosine phosphatase CD45 with an IC50 value of 0.29 μM.{46246} NQ301 (3 mg/kg) inhibits ovalbumin-induced footpad swelling in a mouse model of delayed-type hypersensitivity. It is also active against C. albicans, A. niger, B. subtilis, S. aureus, E. coli, and P. aeruginosa (MICs = 12.5-50 μg/ml).{46247}  

     

    Brand:
    Cayman
    SKU:21958 -

    Out of stock

  • Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death.{10689,26710} NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.{26710} It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.{26712,26711}  

     

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  • Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death.{10689,26710} NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.{26710} It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.{26712,26711}  

     

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    Cayman
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  • Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death.{10689,26710} NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.{26710} It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.{26712,26711}  

     

    Brand:
    Cayman
    SKU:-
  • Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death.{10689,26710} NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.{26710} It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.{26712,26711}  

     

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    Cayman
    SKU:-
  • NQTrp is an inhibitor of Alzheimer’s disease-associated amyloid β (Aβ) oligomerization and fibrillization (IC50 = 50 nM for formation of fibrils from Aβ1-42).{31208,31209} It has been shown to reduce the cytotoxic effect of Aβ oligomers in a cultured neuronal cell line.{31208}  

     

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  • NQTrp is an inhibitor of Alzheimer’s disease-associated amyloid β (Aβ) oligomerization and fibrillization (IC50 = 50 nM for formation of fibrils from Aβ1-42).{31208,31209} It has been shown to reduce the cytotoxic effect of Aβ oligomers in a cultured neuronal cell line.{31208}  

     

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    Cayman
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  • NQTrp is an inhibitor of Alzheimer’s disease-associated amyloid β (Aβ) oligomerization and fibrillization (IC50 = 50 nM for formation of fibrils from Aβ1-42).{31208,31209} It has been shown to reduce the cytotoxic effect of Aβ oligomers in a cultured neuronal cell line.{31208}  

     

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    Cayman
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  • NQTrp is an inhibitor of Alzheimer’s disease-associated amyloid β (Aβ) oligomerization and fibrillization (IC50 = 50 nM for formation of fibrils from Aβ1-42).{31208,31209} It has been shown to reduce the cytotoxic effect of Aβ oligomers in a cultured neuronal cell line.{31208}  

     

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    Cayman
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  • Immunogen: Synthetic peptide from the C-terminal region of human Nrf2 protein • Host: Rabbit • Species Reactivity: (+) Human, mouse, rat • Cross Reactivity: N/A • Applications: FC, ICC, IF, WB • MW = 90 kDa  

     

    Brand:
    Cayman
    SKU:10214- 1 ea
  • Nuclear factor erythroid 2-related factor 2 (Nrf2) is a basic leucine zipper transcription factor encoded by NFE2L2 in humans that regulates the cellular antioxidant response.{53865} It is a 605-amino acid protein comprised of seven highly conserved Nrf2-ECH (Neh) homology domains.{53866,53867} Nrf2 contains a large central domain that recruits transcriptional co-activators, mediates heterodimerization with the transcription factor Maf, and can be phosphorylated by GSK3 or the ubiquitin ligase adapter protein β-TrCP.{53868,53867} The Nrf2 central domain is flanked by an N-terminal Neh2 domain that binds the negative regulator Kelch-like ECH-associated protein 1 (Keap1; Item No. 32035) and a C-terminal Neh3 domain that is required for transactivation.{53867} Nrf2 is ubiquitously expressed and, under homeostatic conditions, associates with Keap1 in the cytoplasm, preventing Nrf2 nuclear translocation and promoting its ubiquitination and proteasomal degradation.{53866,53869} In the presence of xenobiotic electrophiles or oxidants, Keap1 releases Nrf2 which translocates to the nucleus, dimerizes with Maf, and induces the expression of a variety of cytoprotective genes that have antioxidant, anti-inflammatory, and metabolic functions.{53870,53745,53865} Nrf2 siRNA knockdown increases DNA-crosslinking and apoptosis induced by cisplatin (Item No. 13119) in A549 cancer cells, indicating that Nrf2 contributes to chemoresistance.{53871} Tumor Nrf2 levels are increased in patients with non-small cell lung cancer (NSCLC) and this increase is associated with poor overall survival.{53872} Cayman’s Nrf2 (C-Term) Polyclonal Antibody can be used for flow cytometry (FC), immunocytochemistry (ICC), immunofluorescence (IF), and Western blot (WB) applications. The antibody preferentially recognizes polyubiquitinated Nrf2 at 90 kDa from human, mouse, and rat samples.  

     

    Brand:
    Cayman
    SKU:10214 - 1 ea

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  • Immunogen: Synthetic peptide from the C-terminal region of human Nrf2 protein • Host: Rabbit • Species Reactivity: (+) Human, mouse, rat • Cross Reactivity: N/A • Applications: FC, ICC, IF, WB • MW = 90 kDa  

     

    Brand:
    Cayman
    SKU:10214- 1 ea

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  • Nuclear factor erythroid 2-related factor 2 (Nrf2) is a basic leucine zipper transcription factor encoded by NFE2L2 in humans that regulates the cellular antioxidant response.{53865} It is a 605-amino acid protein comprised of seven highly conserved Nrf2-ECH (Neh) homology domains.{53866,53867} Nrf2 contains a large central domain that recruits transcriptional co-activators, mediates heterodimerization with the transcription factor Maf, and can be phosphorylated by GSK3 or the ubiquitin ligase adapter protein β-TrCP.{53867,53868} The Nrf2 central domain is flanked by an N-terminal Neh2 domain that binds the negative regulator Kelch-like ECH-associated protein 1 (Keap1; Item No. 32035) and a C-terminal Neh3 domain that is required for transactivation.{53867} Nrf2 is ubiquitously expressed and, under homeostatic conditions, associates with Keap1 in the cytoplasm, preventing Nrf2 nuclear translocation and promoting its ubiquitination and proteasomal degradation.{53866,53869} In the presence of xenobiotic electrophiles or oxidants, Keap1 releases Nrf2 which translocates to the nucleus, dimerizes with Maf, and induces the expression of a variety of cytoprotective genes that have antioxidant, anti-inflammatory, and metabolic functions.{53865,53870,53745} Nrf2 siRNA knockdown increases DNA-crosslinking and apoptosis induced by cisplatin (Item No. 13119) in A549 cancer cells, indicating that Nrf2 contributes to chemoresistance.{53871} Tumor Nrf2 levels are increased in patients with non-small cell lung cancer (NSCLC) and this increase is associated with poor overall survival.{53872} Cayman’s Nrf2 (N-Term) Polyclonal Antibody can be used for flow cytometry (FC), immunocytochemistry (ICC), and Western blot (WB) applications. The antibody recognizes native and polyubiquitinated Nrf2 at 67 and 90 kDa, respectively, from human, mouse, and rat samples.  

     

    Brand:
    Cayman
    SKU:14114 - 1 ea

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  • Immunogen: Peptide from the N-terminal region of human Nrf2 protein • Host: Rabbit • Species Reactivity: (+) Human, mouse, rat • Applications: FC, ICC, IF, WB • MW = 67 and 90 kDa for native and polyubiquitinated Nrf2, respectively  

     

    Brand:
    Cayman
    SKU:14114- 1 ea

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  • Immunogen: Peptide from the N-terminal region of human Nrf2 protein • Host: Rabbit • Species Reactivity: (+) Human, mouse, rat • Applications: FC, ICC, IF, WB • MW = 67 and 90 kDa for native and polyubiquitinated Nrf2, respectively  

     

    Brand:
    Cayman
    SKU:14114- 1 ea
  • Nuclear factor E2-related factor 2 (Nrf2) is a transcription factor that plays a key role in maintaining redox homeostasis via its interaction with a cysteine-rich protein Kelch-like ECH-associated protein 1 (Keap1). In resting cells, Nrf2 and Keap1 form a tight complex, which is targeted for degradation by proteasomes. Under oxidative stress, Nrf2 is released from the Nrf2/Keap1 complex and translocates to the nucleus where it is able to induce the expression of a battery of genes encoding diverse cytoprotective proteins, including antioxidative enzymes, anti-inflammatory mediators, and proteasomes. Cayman’s Nrf2 Transcription Factor Assay is a non-radioactive, colorimetric method for detecting specific transcription factor DNA binding activity in nuclear extracts. A specific double stranded DNA (dsDNA) sequence containing the Nrf2 response element is immobilized onto the wells of a 96-well plate. Nrf2 contained in nuclear extract samples will bind specifically to the Nrf2 response element and can be detected by addition of a specific Nrf2 antibody and a secondary antibody conjugated to HRP.  

     

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    Cayman
    SKU:600590 - 96 wells

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  • NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa/KCa1.1).{32423} It is selective for BKCa and is thought to bind directly the ɑ subunit.{32423} NS 11021 has been shown to relax intracavernous arterial rings and corpus cavernosum strips in vitro and to enhance erectile responses in intact rats.{32424}  

     

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  • NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa/KCa1.1).{32423} It is selective for BKCa and is thought to bind directly the ɑ subunit.{32423} NS 11021 has been shown to relax intracavernous arterial rings and corpus cavernosum strips in vitro and to enhance erectile responses in intact rats.{32424}  

     

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  • NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa/KCa1.1).{32423} It is selective for BKCa and is thought to bind directly the ɑ subunit.{32423} NS 11021 has been shown to relax intracavernous arterial rings and corpus cavernosum strips in vitro and to enhance erectile responses in intact rats.{32424}  

     

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    Cayman
    SKU:-
  • NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa/KCa1.1).{32423} It is selective for BKCa and is thought to bind directly the ɑ subunit.{32423} NS 11021 has been shown to relax intracavernous arterial rings and corpus cavernosum strips in vitro and to enhance erectile responses in intact rats.{32424}  

     

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  • NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is selective for GABAA receptors containing α1, α2, α3, or α5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α4 or α6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α3 and α5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). In vivo, NS 11394 inhibits the binding of [3H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC50 values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. 92350) injections in a rat model of neuropathic pain.{36346}  

     

    Brand:
    Cayman
    SKU:23872 - 1 mg

    Available on backorder

  • NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is selective for GABAA receptors containing α1, α2, α3, or α5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α4 or α6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α3 and α5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). In vivo, NS 11394 inhibits the binding of [3H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC50 values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. 92350) injections in a rat model of neuropathic pain.{36346}  

     

    Brand:
    Cayman
    SKU:23872 - 10 mg

    Available on backorder

  • NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is selective for GABAA receptors containing α1, α2, α3, or α5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α4 or α6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α3 and α5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). In vivo, NS 11394 inhibits the binding of [3H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC50 values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. 92350) injections in a rat model of neuropathic pain.{36346}  

     

    Brand:
    Cayman
    SKU:23872 - 25 mg

    Available on backorder

  • NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is selective for GABAA receptors containing α1, α2, α3, or α5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α4 or α6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α3 and α5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). In vivo, NS 11394 inhibits the binding of [3H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC50 values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. 92350) injections in a rat model of neuropathic pain.{36346}  

     

    Brand:
    Cayman
    SKU:23872 - 5 mg

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  • NS 1619 is a calcium-dependent activator of large-conductance Ca2+-activated K+ (BKCa) channels in vascular smooth muscle.{30652} It is typically used at a concentration of 30 µM to hyperpolarize the membrane potential of single myocytes during studies of smooth muscle relaxation and vasodilation.{30656,30653} Studies suggest that activation of BKCa channels by NS 1619 can protect the cardiac muscle against pulmonary hypertension as well as ischemia and reperfusion injury in various animal models.{30655,30654}  

     

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  • NS 1619 is a calcium-dependent activator of large-conductance Ca2+-activated K+ (BKCa) channels in vascular smooth muscle.{30652} It is typically used at a concentration of 30 µM to hyperpolarize the membrane potential of single myocytes during studies of smooth muscle relaxation and vasodilation.{30656,30653} Studies suggest that activation of BKCa channels by NS 1619 can protect the cardiac muscle against pulmonary hypertension as well as ischemia and reperfusion injury in various animal models.{30655,30654}  

     

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    Cayman
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  • NS 1619 is a calcium-dependent activator of large-conductance Ca2+-activated K+ (BKCa) channels in vascular smooth muscle.{30652} It is typically used at a concentration of 30 µM to hyperpolarize the membrane potential of single myocytes during studies of smooth muscle relaxation and vasodilation.{30656,30653} Studies suggest that activation of BKCa channels by NS 1619 can protect the cardiac muscle against pulmonary hypertension as well as ischemia and reperfusion injury in various animal models.{30655,30654}  

     

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    SKU:-

    Available on backorder

  • NS 1619 is a calcium-dependent activator of large-conductance Ca2+-activated K+ (BKCa) channels in vascular smooth muscle.{30652} It is typically used at a concentration of 30 µM to hyperpolarize the membrane potential of single myocytes during studies of smooth muscle relaxation and vasodilation.{30656,30653} Studies suggest that activation of BKCa channels by NS 1619 can protect the cardiac muscle against pulmonary hypertension as well as ischemia and reperfusion injury in various animal models.{30655,30654}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NS 1643 is an activator of the human ether-a-go-go related gene (ERG1, KCNH2, hERG) KV11.1 channel (EC50 = 10.5 μM).{32589,32591} It also activates the KV11.2 (ERG2, KCNH6) channel, but evokes a distinctly different response from that of KV11.1.{32590} NS 1643 is commonly used in cells or isolated tissues.{32589,32591,32592}  

     

    Brand:
    Cayman
    SKU:20343 -

    Available on backorder

  • NS 1643 is an activator of the human ether-a-go-go related gene (ERG1, KCNH2, hERG) KV11.1 channel (EC50 = 10.5 μM).{32589,32591} It also activates the KV11.2 (ERG2, KCNH6) channel, but evokes a distinctly different response from that of KV11.1.{32590} NS 1643 is commonly used in cells or isolated tissues.{32589,32591,32592}  

     

    Brand:
    Cayman
    SKU:20343 -

    Available on backorder

  • NS 1643 is an activator of the human ether-a-go-go related gene (ERG1, KCNH2, hERG) KV11.1 channel (EC50 = 10.5 μM).{32589,32591} It also activates the KV11.2 (ERG2, KCNH6) channel, but evokes a distinctly different response from that of KV11.1.{32590} NS 1643 is commonly used in cells or isolated tissues.{32589,32591,32592}  

     

    Brand:
    Cayman
    SKU:20343 -

    Available on backorder

  • NS 1643 is an activator of the human ether-a-go-go related gene (ERG1, KCNH2, hERG) KV11.1 channel (EC50 = 10.5 μM).{32589,32591} It also activates the KV11.2 (ERG2, KCNH6) channel, but evokes a distinctly different response from that of KV11.1.{32590} NS 1643 is commonly used in cells or isolated tissues.{32589,32591,32592}  

     

    Brand:
    Cayman
    SKU:20343 -

    Available on backorder

  • NS 1738 is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs).{29720} When applied in the presence of ACh, NS 1738 increases the peak amplitude of the current flowing through α7-containing nAChRs (EC50 = 3.4 µM).{29720} NS 1738 displays no substantial activity for α4β2-, α3β3-, and α1-containing receptors. It is modestly brain-penetrant and counteracts (-)-scopolamine-induced deficit in acquisition of a water-maze learning task in rats.{29720} NS 1738 also improves performance in the rat social recognition test.{29720} NS 1738 is used to selectively evaluate the role of α7-containing nAChRs in signaling pathways.{33287,33288}  

     

    Brand:
    Cayman
    SKU:21018 -

    Out of stock

  • NS 1738 is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs).{29720} When applied in the presence of ACh, NS 1738 increases the peak amplitude of the current flowing through α7-containing nAChRs (EC50 = 3.4 µM).{29720} NS 1738 displays no substantial activity for α4β2-, α3β3-, and α1-containing receptors. It is modestly brain-penetrant and counteracts (-)-scopolamine-induced deficit in acquisition of a water-maze learning task in rats.{29720} NS 1738 also improves performance in the rat social recognition test.{29720} NS 1738 is used to selectively evaluate the role of α7-containing nAChRs in signaling pathways.{33287,33288}  

     

    Brand:
    Cayman
    SKU:21018 -

    Out of stock

  • NS 1738 is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs).{29720} When applied in the presence of ACh, NS 1738 increases the peak amplitude of the current flowing through α7-containing nAChRs (EC50 = 3.4 µM).{29720} NS 1738 displays no substantial activity for α4β2-, α3β3-, and α1-containing receptors. It is modestly brain-penetrant and counteracts (-)-scopolamine-induced deficit in acquisition of a water-maze learning task in rats.{29720} NS 1738 also improves performance in the rat social recognition test.{29720} NS 1738 is used to selectively evaluate the role of α7-containing nAChRs in signaling pathways.{33287,33288}  

     

    Brand:
    Cayman
    SKU:21018 -

    Out of stock

  • NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1; IC50 = 9.4 nM in HEK293 cells expressing the human channel).{43059} It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Item No. 11016) (IC50s = 14, 15, and 9 nM, respectively). NS 6180 is selective for IKCa1/KCa3.1 over voltage-gated sodium (Nav) and most voltage-gated potassium channels (Kv) but does inhibit KCa1.1, Kv1.3, and Kv11.1 channels by greater than 50% at 10 µM. It is selective for potassium channels over G protein-coupled receptors and ion channels, inhibiting only the norepinephrine and dopamine transporters, L-type calcium channel, and melatonin receptor MT1 by greater than 50% in a panel of 69 receptors and channels. NS 6180 inhibits T-lymphocyte activation and the release of the Th1 cytokines IL-2 and IFN-γ in vitro (IC50 = ~50 nM). It also increases proliferation of natural killer (NK) cells and selectively increases cytotoxicity of adherent, but not non-adherent, NK cells.{43560} In a rat model of inflammatory bowel disease (IBD) induced by DNBS, NS 6180 (3 and 10 mg/kg per day) decreases colon inflammation and improves weight gain.{43059}  

     

    Brand:
    Cayman
    SKU:-
  • NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1; IC50 = 9.4 nM in HEK293 cells expressing the human channel).{43059} It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Item No. 11016) (IC50s = 14, 15, and 9 nM, respectively). NS 6180 is selective for IKCa1/KCa3.1 over voltage-gated sodium (Nav) and most voltage-gated potassium channels (Kv) but does inhibit KCa1.1, Kv1.3, and Kv11.1 channels by greater than 50% at 10 µM. It is selective for potassium channels over G protein-coupled receptors and ion channels, inhibiting only the norepinephrine and dopamine transporters, L-type calcium channel, and melatonin receptor MT1 by greater than 50% in a panel of 69 receptors and channels. NS 6180 inhibits T-lymphocyte activation and the release of the Th1 cytokines IL-2 and IFN-γ in vitro (IC50 = ~50 nM). It also increases proliferation of natural killer (NK) cells and selectively increases cytotoxicity of adherent, but not non-adherent, NK cells.{43560} In a rat model of inflammatory bowel disease (IBD) induced by DNBS, NS 6180 (3 and 10 mg/kg per day) decreases colon inflammation and improves weight gain.{43059}  

     

    Brand:
    Cayman
    SKU:-
  • NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1; IC50 = 9.4 nM in HEK293 cells expressing the human channel).{43059} It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Item No. 11016) (IC50s = 14, 15, and 9 nM, respectively). NS 6180 is selective for IKCa1/KCa3.1 over voltage-gated sodium (Nav) and most voltage-gated potassium channels (Kv) but does inhibit KCa1.1, Kv1.3, and Kv11.1 channels by greater than 50% at 10 µM. It is selective for potassium channels over G protein-coupled receptors and ion channels, inhibiting only the norepinephrine and dopamine transporters, L-type calcium channel, and melatonin receptor MT1 by greater than 50% in a panel of 69 receptors and channels. NS 6180 inhibits T-lymphocyte activation and the release of the Th1 cytokines IL-2 and IFN-γ in vitro (IC50 = ~50 nM). It also increases proliferation of natural killer (NK) cells and selectively increases cytotoxicity of adherent, but not non-adherent, NK cells.{43560} In a rat model of inflammatory bowel disease (IBD) induced by DNBS, NS 6180 (3 and 10 mg/kg per day) decreases colon inflammation and improves weight gain.{43059}  

     

    Brand:
    Cayman
    SKU:-
  • NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1; IC50 = 9.4 nM in HEK293 cells expressing the human channel).{43059} It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Item No. 11016) (IC50s = 14, 15, and 9 nM, respectively). NS 6180 is selective for IKCa1/KCa3.1 over voltage-gated sodium (Nav) and most voltage-gated potassium channels (Kv) but does inhibit KCa1.1, Kv1.3, and Kv11.1 channels by greater than 50% at 10 µM. It is selective for potassium channels over G protein-coupled receptors and ion channels, inhibiting only the norepinephrine and dopamine transporters, L-type calcium channel, and melatonin receptor MT1 by greater than 50% in a panel of 69 receptors and channels. NS 6180 inhibits T-lymphocyte activation and the release of the Th1 cytokines IL-2 and IFN-γ in vitro (IC50 = ~50 nM). It also increases proliferation of natural killer (NK) cells and selectively increases cytotoxicity of adherent, but not non-adherent, NK cells.{43560} In a rat model of inflammatory bowel disease (IBD) induced by DNBS, NS 6180 (3 and 10 mg/kg per day) decreases colon inflammation and improves weight gain.{43059}  

     

    Brand:
    Cayman
    SKU:-
  • NS 8593 is an inhibitory gating modifier of small conductance calcium-activated potassium (SK) channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for SK channels over intermediate (IK) and large conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}  

     

    Brand:
    Cayman
    SKU:29774 - 1 mg

    Available on backorder

  • NS 8593 is an inhibitory gating modifier of small conductance calcium-activated potassium (SK) channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for SK channels over intermediate (IK) and large conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}  

     

    Brand:
    Cayman
    SKU:29774 - 10 mg

    Available on backorder

  • NS 8593 is an inhibitory gating modifier of small conductance calcium-activated potassium (SK) channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for SK channels over intermediate (IK) and large conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}  

     

    Brand:
    Cayman
    SKU:29774 - 25 mg

    Available on backorder

  • NS 8593 is an inhibitory gating modifier of small conductance calcium-activated potassium (SK) channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for SK channels over intermediate (IK) and large conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}  

     

    Brand:
    Cayman
    SKU:29774 - 5 mg

    Available on backorder

  • NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM).{53135} In vivo, NS 9283 potentiates ABT-594 (Item No. 22822) analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis.{53136} It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.{53137}  

     

    Brand:
    Cayman
    SKU:29189 - 1 mg

    Available on backorder

  • NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM).{53135} In vivo, NS 9283 potentiates ABT-594 (Item No. 22822) analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis.{53136} It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.{53137}  

     

    Brand:
    Cayman
    SKU:29189 - 10 mg

    Available on backorder

  • NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM).{53135} In vivo, NS 9283 potentiates ABT-594 (Item No. 22822) analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis.{53136} It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.{53137}  

     

    Brand:
    Cayman
    SKU:29189 - 25 mg

    Available on backorder

  • NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM).{53135} In vivo, NS 9283 potentiates ABT-594 (Item No. 22822) analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis.{53136} It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.{53137}  

     

    Brand:
    Cayman
    SKU:29189 - 5 mg

    Available on backorder

  • NS-2028 is a specific inhibitor of soluble guanylyl cyclase. It inhibits purified bovine lung guanylyl cyclase in a concentration dependent and irreversible manner with IC50 values of 30 and 200 nM for basal and NO-stimulated enzymes, respectively.{6642} S-nitroso-glutathione-enhanced guanylyl cyclase activity in mouse cerebellum homogenates is inhibited by NS-2028 with an IC50 value of 17 nM, making it about 4.7 fold more potent than ODQ, which has an IC50 value of 80 nM for inhibition of soluble guanylyl cyclase in the same assay.{6642} NS-2028 does not inhibit particulate guanylyl cyclase or adenylyl cyclase.  

     

    Brand:
    Cayman
    SKU:81600 - 1 mg

    Available on backorder

  • NS-2028 is a specific inhibitor of soluble guanylyl cyclase. It inhibits purified bovine lung guanylyl cyclase in a concentration dependent and irreversible manner with IC50 values of 30 and 200 nM for basal and NO-stimulated enzymes, respectively.{6642} S-nitroso-glutathione-enhanced guanylyl cyclase activity in mouse cerebellum homogenates is inhibited by NS-2028 with an IC50 value of 17 nM, making it about 4.7 fold more potent than ODQ, which has an IC50 value of 80 nM for inhibition of soluble guanylyl cyclase in the same assay.{6642} NS-2028 does not inhibit particulate guanylyl cyclase or adenylyl cyclase.  

     

    Brand:
    Cayman
    SKU:81600 - 10 mg

    Available on backorder

  • NS-2028 is a specific inhibitor of soluble guanylyl cyclase. It inhibits purified bovine lung guanylyl cyclase in a concentration dependent and irreversible manner with IC50 values of 30 and 200 nM for basal and NO-stimulated enzymes, respectively.{6642} S-nitroso-glutathione-enhanced guanylyl cyclase activity in mouse cerebellum homogenates is inhibited by NS-2028 with an IC50 value of 17 nM, making it about 4.7 fold more potent than ODQ, which has an IC50 value of 80 nM for inhibition of soluble guanylyl cyclase in the same assay.{6642} NS-2028 does not inhibit particulate guanylyl cyclase or adenylyl cyclase.  

     

    Brand:
    Cayman
    SKU:81600 - 25 mg

    Available on backorder

  • NS-2028 is a specific inhibitor of soluble guanylyl cyclase. It inhibits purified bovine lung guanylyl cyclase in a concentration dependent and irreversible manner with IC50 values of 30 and 200 nM for basal and NO-stimulated enzymes, respectively.{6642} S-nitroso-glutathione-enhanced guanylyl cyclase activity in mouse cerebellum homogenates is inhibited by NS-2028 with an IC50 value of 17 nM, making it about 4.7 fold more potent than ODQ, which has an IC50 value of 80 nM for inhibition of soluble guanylyl cyclase in the same assay.{6642} NS-2028 does not inhibit particulate guanylyl cyclase or adenylyl cyclase.  

     

    Brand:
    Cayman
    SKU:81600 - 5 mg

    Available on backorder

  • Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.{14998}  

     

    Brand:
    Cayman
    SKU:10010411 - 1 mg

    Available on backorder

  • Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.{14998}  

     

    Brand:
    Cayman
    SKU:10010411 - 10 mg

    Available on backorder

  • Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.{14998}  

     

    Brand:
    Cayman
    SKU:10010411 - 5 mg

    Available on backorder

  • Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.{14998}  

     

    Brand:
    Cayman
    SKU:10010411 - 50 mg

    Available on backorder

  • NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 µM, respectively.{1286} The IC50 values for ovine COX-1 and -2 are 220 and 0.15 µM, respectively.{1364}  

     

    Brand:
    Cayman
    SKU:70590 - 10 mg

    Available on backorder

  • NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 µM, respectively.{1286} The IC50 values for ovine COX-1 and -2 are 220 and 0.15 µM, respectively.{1364}  

     

    Brand:
    Cayman
    SKU:70590 - 25 mg

    Available on backorder

  • NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 µM, respectively.{1286} The IC50 values for ovine COX-1 and -2 are 220 and 0.15 µM, respectively.{1364}  

     

    Brand:
    Cayman
    SKU:70590 - 5 mg

    Available on backorder

  • NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 µM, respectively.{1286} The IC50 values for ovine COX-1 and -2 are 220 and 0.15 µM, respectively.{1364}  

     

    Brand:
    Cayman
    SKU:70590 - 50 mg

    Available on backorder

  • NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels).{27789,25556} It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels.{27789,25556,27794} NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects.{27789,25556} It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO (Item No. 14575) and often used in conjunction with CyPPA (Item No. 15614) to distinguish between SK1 and SK3 subtypes.{27789,25556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels).{27789,25556} It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels.{27789,25556,27794} NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects.{27789,25556} It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO (Item No. 14575) and often used in conjunction with CyPPA (Item No. 15614) to distinguish between SK1 and SK3 subtypes.{27789,25556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels).{27789,25556} It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels.{27789,25556,27794} NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects.{27789,25556} It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO (Item No. 14575) and often used in conjunction with CyPPA (Item No. 15614) to distinguish between SK1 and SK3 subtypes.{27789,25556}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}  

     

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    Cayman
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  • Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}  

     

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    Cayman
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  • NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}  

     

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    Cayman
    SKU:19811 -

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  • NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}  

     

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    Cayman
    SKU:19811 -

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  • NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}  

     

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    Cayman
    SKU:19811 -

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  • NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}  

     

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    Cayman
    SKU:19811 -

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  • NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}  

     

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    Cayman
    SKU:20117 -

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  • NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}  

     

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    Cayman
    SKU:20117 -

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  • NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}  

     

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    Cayman
    SKU:20117 -

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  • NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}  

     

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    Cayman
    SKU:20117 -

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  • NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}  

     

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    Cayman
    SKU:-

    Out of stock

  • NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}  

     

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    Cayman
    SKU:-

    Out of stock

  • NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}  

     

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    Cayman
    SKU:-

    Out of stock

  • NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.  

     

    Brand:
    Cayman
    SKU:26020 - 1 mg

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  • NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.  

     

    Brand:
    Cayman
    SKU:26020 - 10 mg

    Available on backorder

  • NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.  

     

    Brand:
    Cayman
    SKU:26020 - 25 mg

    Available on backorder

  • NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.  

     

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    Cayman
    SKU:26020 - 5 mg

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  • NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.{37384} It inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells. NSC 185058 (100 µM) reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells. It decreases phosphorylation of ribosomal protein S6 (RPS6) only marginally and does not affect phosphatidylinositol 3-kinase (PI3K) activity, indicating a direct role on ATG4B rather than through the mammalian target of rapamycin (mTOR) and PI3K signaling pathways. NSC 185058 (100 mg/kg) decreases autophagic vacuoles in vivo in mouse liver, inhibits tumor growth in an osteosarcoma nude mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors.  

     

    Brand:
    Cayman
    SKU:23957 - 1 mg

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  • NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.{37384} It inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells. NSC 185058 (100 µM) reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells. It decreases phosphorylation of ribosomal protein S6 (RPS6) only marginally and does not affect phosphatidylinositol 3-kinase (PI3K) activity, indicating a direct role on ATG4B rather than through the mammalian target of rapamycin (mTOR) and PI3K signaling pathways. NSC 185058 (100 mg/kg) decreases autophagic vacuoles in vivo in mouse liver, inhibits tumor growth in an osteosarcoma nude mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors.  

     

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    Cayman
    SKU:23957 - 5 mg

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  • NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}  

     

    Brand:
    Cayman
    SKU:27949 - 1 mg

    Available on backorder

  • NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}  

     

    Brand:
    Cayman
    SKU:27949 - 10 mg

    Available on backorder

  • NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}  

     

    Brand:
    Cayman
    SKU:27949 - 25 mg

    Available on backorder

  • NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}  

     

    Brand:
    Cayman
    SKU:27949 - 5 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}  

     

    Brand:
    Cayman
    SKU:10011255 - 1 mg

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  • Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}  

     

    Brand:
    Cayman
    SKU:10011255 - 10 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}  

     

    Brand:
    Cayman
    SKU:10011255 - 5 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}  

     

    Brand:
    Cayman
    SKU:10011255 - 50 mg

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  • NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}  

     

    Brand:
    Cayman
    SKU:28856 - 10 mg

    Available on backorder

  • NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}  

     

    Brand:
    Cayman
    SKU:28856 - 25 mg

    Available on backorder

  • NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}  

     

    Brand:
    Cayman
    SKU:28856 - 5 mg

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  • NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.  

     

    Brand:
    Cayman
    SKU:23327 - 1 mg

    Available on backorder

  • NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.  

     

    Brand:
    Cayman
    SKU:23327 - 10 mg

    Available on backorder

  • NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.  

     

    Brand:
    Cayman
    SKU:23327 - 5 mg

    Available on backorder

  • Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}  

     

    Brand:
    Cayman
    SKU:-
  • Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}  

     

    Brand:
    Cayman
    SKU:-
  • Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}  

     

    Brand:
    Cayman
    SKU:-
  • Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}  

     

    Brand:
    Cayman
    SKU:-
  • NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.  

     

    Brand:
    Cayman
    SKU:21947 -

    Out of stock

  • NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.  

     

    Brand:
    Cayman
    SKU:21947 -

    Out of stock

  • NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.  

     

    Brand:
    Cayman
    SKU:21947 -

    Out of stock

  • NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.  

     

    Brand:
    Cayman
    SKU:21947 -

    Out of stock

  • NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.  

     

    Brand:
    Cayman
    SKU:9002543 - 1 mg

    Available on backorder

  • NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.  

     

    Brand:
    Cayman
    SKU:9002543 - 10 mg

    Available on backorder

  • NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.  

     

    Brand:
    Cayman
    SKU:9002543 - 25 mg

    Available on backorder

  • NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.  

     

    Brand:
    Cayman
    SKU:9002543 - 5 mg

    Available on backorder

  • NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}  

     

    Brand:
    Cayman
    SKU:23701 - 10 mg

    Available on backorder

  • NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}  

     

    Brand:
    Cayman
    SKU:23701 - 25 mg

    Available on backorder

  • NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}  

     

    Brand:
    Cayman
    SKU:23701 - 5 mg

    Available on backorder

  • Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}  

     

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    Cayman
    SKU:-

    Out of stock

  • Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}  

     

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    Cayman
    SKU:-

    Out of stock

  • Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}  

     

    Brand:
    Cayman
    SKU:23443 - 10 mg

    Available on backorder

  • NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}  

     

    Brand:
    Cayman
    SKU:23443 - 25 mg

    Available on backorder

  • NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}  

     

    Brand:
    Cayman
    SKU:23443 - 5 mg

    Available on backorder

  • NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}  

     

    Brand:
    Cayman
    SKU:23443 - 50 mg

    Available on backorder

  • NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}  

     

    Brand:
    Cayman
    SKU:19919 -

    Available on backorder

  • NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}  

     

    Brand:
    Cayman
    SKU:19919 -

    Available on backorder

  • NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}  

     

    Brand:
    Cayman
    SKU:19919 -

    Available on backorder

  • NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}  

     

    Brand:
    Cayman
    SKU:19919 -

    Available on backorder

  • NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.  

     

    Brand:
    Cayman
    SKU:21973 -

    Out of stock

  • NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.  

     

    Brand:
    Cayman
    SKU:21973 -

    Out of stock

  • NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.  

     

    Brand:
    Cayman
    SKU:21973 -

    Out of stock

  • NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.  

     

    Brand:
    Cayman
    SKU:21973 -

    Out of stock

  • NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}  

     

    Brand:
    Cayman
    SKU:20569 -

    Available on backorder

  • NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}  

     

    Brand:
    Cayman
    SKU:20569 -

    Available on backorder

  • NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}  

     

    Brand:
    Cayman
    SKU:20569 -

    Available on backorder

  • NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}  

     

    Brand:
    Cayman
    SKU:20569 -

    Available on backorder

  • 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 various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • 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 various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • 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 various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • 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 various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).{17980} NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).{17980,17978} By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,{17979,17981} arrests cells at both G1 and G2/M phases,{17979} and prevents the proliferation of several human tumor cell lines.{17980,17979,17982}  

     

    Brand:
    Cayman
    SKU:-