Chemicals

Showing 23101–23250 of 41137 results

  • Ivermectin B1a monosaccharide is produced by selective hydrolysis of the terminal saccharide unit of ivermectin.{31087} It can inhibit nematode larval development, but does not cause paralytic activity. This compound has been used as a probe to detect some types of ivermectin resistance.{31085}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ivermectin B1b is the minor component (1a (>80%; Item No. 18768).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}  

     

    Brand:
    Cayman
    SKU:23824 - 2.5 mg

    Available on backorder

  • Ivermectin B1b is the minor component (1a (>80%; Item No. 18768).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}  

     

    Brand:
    Cayman
    SKU:23824 - 500 µg

    Available on backorder

  • IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.  

     

    Brand:
    Cayman
    SKU:22729 -

    Out of stock

  • IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.  

     

    Brand:
    Cayman
    SKU:22729 -

    Out of stock

  • IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.  

     

    Brand:
    Cayman
    SKU:22729 -

    Out of stock

  • IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.  

     

    Brand:
    Cayman
    SKU:22729 -

    Out of stock

  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}  

     

    Brand:
    Cayman
    SKU:-
  • IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}  

     

    Brand:
    Cayman
    SKU:-
  • IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}  

     

    Brand:
    Cayman
    SKU:-
  • IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}  

     

    Brand:
    Cayman
    SKU:-
  • IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}  

     

    Brand:
    Cayman
    SKU:-
  • Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}  

     

    Brand:
    Cayman
    SKU:-
  • Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}  

     

    Brand:
    Cayman
    SKU:-
  • Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM.{17505} It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.{17505} The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.{17948} In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.{17948} The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM.{17505} It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.{17505} The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.{17948} In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.{17948} The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM.{17505} It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.{17505} The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.{17948} In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.{17948} The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM.{17505} It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.{17505} The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.{17948} In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.{17948} The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.{17505}  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis,{17947} and tumorigenesis.{14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-exo is a diastereomer of IWR-1-endo, the potent inhibitor of the Wnt response.{17505} Whereas IWR-1-endo strongly blocks cell-based Wnt/β-catenin pathway reporter response (IC50 = 180 nM){17505} and suppresses Wnt-dependent zebrafish tail fin regeneration (0.5 μM),{17948} IWR-1-exo has little effect in either assay at 10 μM.{17505} Thus, this compound is an ideal control for tests involving the active form, IWR-1-endo.  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis,{17947} and tumorigenesis.{14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-exo is a diastereomer of IWR-1-endo, the potent inhibitor of the Wnt response.{17505} Whereas IWR-1-endo strongly blocks cell-based Wnt/β-catenin pathway reporter response (IC50 = 180 nM){17505} and suppresses Wnt-dependent zebrafish tail fin regeneration (0.5 μM),{17948} IWR-1-exo has little effect in either assay at 10 μM.{17505} Thus, this compound is an ideal control for tests involving the active form, IWR-1-endo.  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis,{17947} and tumorigenesis.{14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-exo is a diastereomer of IWR-1-endo, the potent inhibitor of the Wnt response.{17505} Whereas IWR-1-endo strongly blocks cell-based Wnt/β-catenin pathway reporter response (IC50 = 180 nM){17505} and suppresses Wnt-dependent zebrafish tail fin regeneration (0.5 μM),{17948} IWR-1-exo has little effect in either assay at 10 μM.{17505} Thus, this compound is an ideal control for tests involving the active form, IWR-1-endo.  

     

    Brand:
    Cayman
    SKU:-
  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis,{17947} and tumorigenesis.{14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-exo is a diastereomer of IWR-1-endo, the potent inhibitor of the Wnt response.{17505} Whereas IWR-1-endo strongly blocks cell-based Wnt/β-catenin pathway reporter response (IC50 = 180 nM){17505} and suppresses Wnt-dependent zebrafish tail fin regeneration (0.5 μM),{17948} IWR-1-exo has little effect in either assay at 10 μM.{17505} Thus, this compound is an ideal control for tests involving the active form, IWR-1-endo.  

     

    Brand:
    Cayman
    SKU:-
  • Ixabepilone is an epothilone with broad-spectrum anticancer activity against a panel of 21 cancer cell lines (IC50s = 1.4-34.5 nM).{42060} It stabilizes and induces the polymerization of microtubules and induces cell cycle arrest during mitosis. Ixabepilone is cytotoxic to HCT116/VM46 and A2780Tax clonogenic cells, which are resistant to paclitaxel (Item No. 10461; IC90s = 16 and 12.3 nM, respectively, for colony growth inhibition). In vivo, ixabepilone (6.3 and 10 mg/kg, i.v., respectively) shows antitumor activity in paclitaxel-resistant human Pat-21 breast carcinoma and HCT116/VM46 colon carcinoma mouse xenograft models with log cell kill (LCK) values of 1.6 and 2.4, respectively. Ixabepilone (10 mg/kg, i.v.) also increases the time for tumors to quadruple in volume by 7.2, 9, 6.5, 4.7, and >10 weeks, respectively, in mice implanted with Rh18 rhabdomyosarcoma, NB1643 neuroblastoma, WT5 Wilms’ tumor, OS29 osteosarcoma, and BT29 brain carcinoma cells.{42061} Formulations containing ixabepilone have used in the treatment of metastatic breast cancer.{26908}  

     

    Brand:
    Cayman
    SKU:23732 - 1 mg

    Available on backorder

  • Ixabepilone is an epothilone with broad-spectrum anticancer activity against a panel of 21 cancer cell lines (IC50s = 1.4-34.5 nM).{42060} It stabilizes and induces the polymerization of microtubules and induces cell cycle arrest during mitosis. Ixabepilone is cytotoxic to HCT116/VM46 and A2780Tax clonogenic cells, which are resistant to paclitaxel (Item No. 10461; IC90s = 16 and 12.3 nM, respectively, for colony growth inhibition). In vivo, ixabepilone (6.3 and 10 mg/kg, i.v., respectively) shows antitumor activity in paclitaxel-resistant human Pat-21 breast carcinoma and HCT116/VM46 colon carcinoma mouse xenograft models with log cell kill (LCK) values of 1.6 and 2.4, respectively. Ixabepilone (10 mg/kg, i.v.) also increases the time for tumors to quadruple in volume by 7.2, 9, 6.5, 4.7, and >10 weeks, respectively, in mice implanted with Rh18 rhabdomyosarcoma, NB1643 neuroblastoma, WT5 Wilms’ tumor, OS29 osteosarcoma, and BT29 brain carcinoma cells.{42061} Formulations containing ixabepilone have used in the treatment of metastatic breast cancer.{26908}  

     

    Brand:
    Cayman
    SKU:23732 - 10 mg

    Available on backorder

  • Ixabepilone is an epothilone with broad-spectrum anticancer activity against a panel of 21 cancer cell lines (IC50s = 1.4-34.5 nM).{42060} It stabilizes and induces the polymerization of microtubules and induces cell cycle arrest during mitosis. Ixabepilone is cytotoxic to HCT116/VM46 and A2780Tax clonogenic cells, which are resistant to paclitaxel (Item No. 10461; IC90s = 16 and 12.3 nM, respectively, for colony growth inhibition). In vivo, ixabepilone (6.3 and 10 mg/kg, i.v., respectively) shows antitumor activity in paclitaxel-resistant human Pat-21 breast carcinoma and HCT116/VM46 colon carcinoma mouse xenograft models with log cell kill (LCK) values of 1.6 and 2.4, respectively. Ixabepilone (10 mg/kg, i.v.) also increases the time for tumors to quadruple in volume by 7.2, 9, 6.5, 4.7, and >10 weeks, respectively, in mice implanted with Rh18 rhabdomyosarcoma, NB1643 neuroblastoma, WT5 Wilms’ tumor, OS29 osteosarcoma, and BT29 brain carcinoma cells.{42061} Formulations containing ixabepilone have used in the treatment of metastatic breast cancer.{26908}  

     

    Brand:
    Cayman
    SKU:23732 - 5 mg

    Available on backorder

  • Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants.{30028} Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid (Item No. 90220). Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM).{30024,25889,30026} It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress.{25889,30026} Jacaric acid is metabolized in vivo to conjugated linoleic acid (Item No. 90140), which is also cytotoxic to cancer cells.{6849} Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 µM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.{30027,30029}  

     

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    Cayman
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  • Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants.{30028} Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid (Item No. 90220). Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM).{30024,25889,30026} It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress.{25889,30026} Jacaric acid is metabolized in vivo to conjugated linoleic acid (Item No. 90140), which is also cytotoxic to cancer cells.{6849} Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 µM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.{30027,30029}  

     

    Brand:
    Cayman
    SKU:-
  • Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants.{30028} Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid (Item No. 90220). Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM).{30024,25889,30026} It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress.{25889,30026} Jacaric acid is metabolized in vivo to conjugated linoleic acid (Item No. 90140), which is also cytotoxic to cancer cells.{6849} Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 µM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.{30027,30029}  

     

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    Cayman
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  • Jaceosidin is a natural methylated trihydroxyflavone first isolated from plants of the Compositae family. Like many flavones, jaceosidin has antioxidative actions on cells in culture.{34078} It induces cell cycle arrest and apoptosis in cancer cells, suggesting potential roles in cancer therapy.{34079,34080,34081} Jaceosidin also blocks cell signaling related to inflammation, including activation of NF-κB and induced expression of cyclooxygenase 1, inducible nitric oxide synthase, and matrix metalloproteinase-9.{34078,34077}  

     

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    Cayman
    SKU:19758 -

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  • Jaceosidin is a natural methylated trihydroxyflavone first isolated from plants of the Compositae family. Like many flavones, jaceosidin has antioxidative actions on cells in culture.{34078} It induces cell cycle arrest and apoptosis in cancer cells, suggesting potential roles in cancer therapy.{34079,34080,34081} Jaceosidin also blocks cell signaling related to inflammation, including activation of NF-κB and induced expression of cyclooxygenase 1, inducible nitric oxide synthase, and matrix metalloproteinase-9.{34078,34077}  

     

    Brand:
    Cayman
    SKU:19758 -

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  • Jaceosidin is a natural methylated trihydroxyflavone first isolated from plants of the Compositae family. Like many flavones, jaceosidin has antioxidative actions on cells in culture.{34078} It induces cell cycle arrest and apoptosis in cancer cells, suggesting potential roles in cancer therapy.{34079,34080,34081} Jaceosidin also blocks cell signaling related to inflammation, including activation of NF-κB and induced expression of cyclooxygenase 1, inducible nitric oxide synthase, and matrix metalloproteinase-9.{34078,34077}  

     

    Brand:
    Cayman
    SKU:19758 -

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  • Jaceosidin is a natural methylated trihydroxyflavone first isolated from plants of the Compositae family. Like many flavones, jaceosidin has antioxidative actions on cells in culture.{34078} It induces cell cycle arrest and apoptosis in cancer cells, suggesting potential roles in cancer therapy.{34079,34080,34081} Jaceosidin also blocks cell signaling related to inflammation, including activation of NF-κB and induced expression of cyclooxygenase 1, inducible nitric oxide synthase, and matrix metalloproteinase-9.{34078,34077}  

     

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    Cayman
    SKU:19758 -

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  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM – > 10 μM) for other protein tyrosine kinases.{24837} It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.{24837} In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.{24838}  

     

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    Cayman
    SKU:-
  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM – > 10 μM) for other protein tyrosine kinases.{24837} It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.{24837} In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.{24838}  

     

    Brand:
    Cayman
    SKU:-
  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM – > 10 μM) for other protein tyrosine kinases.{24837} It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.{24837} In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.{24838}  

     

    Brand:
    Cayman
    SKU:-
  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM – > 10 μM) for other protein tyrosine kinases.{24837} It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.{24837} In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.{24838}  

     

    Brand:
    Cayman
    SKU:-
  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 in which a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} JAK2 Inhibitor V is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM.{30753} It has no effect on Tyk2 or c-Src kinase function. JAK2 Inhibitor V blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.{30753}  

     

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    Cayman
    SKU:-

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  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 in which a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} JAK2 Inhibitor V is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM.{30753} It has no effect on Tyk2 or c-Src kinase function. JAK2 Inhibitor V blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.{30753}  

     

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    Cayman
    SKU:-

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  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 in which a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} JAK2 Inhibitor V is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM.{30753} It has no effect on Tyk2 or c-Src kinase function. JAK2 Inhibitor V blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.{30753}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 in which a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} JAK2 Inhibitor V is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM.{30753} It has no effect on Tyk2 or c-Src kinase function. JAK2 Inhibitor V blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.{30753}  

     

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    Cayman
    SKU:-

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  • Janthitrem A is a mycotoxin that has been found in P. janthinellum.{46811} It induces tremors in mice and decreases the time to fall from the rotarod when administered at a dose of 4 mg/kg.{46812} Janthitrem A (20 µg/g) also reduces W. cervinata larvae weight gain and food consumption.  

     

    Brand:
    Cayman
    SKU:30166 - 2.5 mg

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  • Janthitrem A is a mycotoxin that has been found in P. janthinellum.{46811} It induces tremors in mice and decreases the time to fall from the rotarod when administered at a dose of 4 mg/kg.{46812} Janthitrem A (20 µg/g) also reduces W. cervinata larvae weight gain and food consumption.  

     

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    Cayman
    SKU:30166 - 500 µg

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  • Jasplakinolide is a natural macrocyclic peptide first isolated from a marine sponge. It potently inhibits the proliferation of PC3 prostate carcinoma cells (IC50 = 35 nM) by binding F-actin (KD = 15 nM).{22599} This binding of jasplakinolide to actin, which is competitive with phalloidin, stabilizes actin filaments in vitro but disrupts actin filaments and induces irregular polymerization of monomeric actin in vivo.{22599,22598} This compound is used to investigate the role of actin in diverse cellular roles, such as motility, transport, and development.{22600,22601}  

     

    Brand:
    Cayman
    SKU:11705 - 100 µg

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  • Jasplakinolide is a natural macrocyclic peptide first isolated from a marine sponge. It potently inhibits the proliferation of PC3 prostate carcinoma cells (IC50 = 35 nM) by binding F-actin (KD = 15 nM).{22599} This binding of jasplakinolide to actin, which is competitive with phalloidin, stabilizes actin filaments in vitro but disrupts actin filaments and induces irregular polymerization of monomeric actin in vivo.{22599,22598} This compound is used to investigate the role of actin in diverse cellular roles, such as motility, transport, and development.{22600,22601}  

     

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    Cayman
    SKU:11705 - 50 µg

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  • Jatrorrhizine is an alkaloid that has been found in the Chinese herb C. chinensis and has diverse biological activities.{45262,45263,45264,45265} It is active against P. falciparum (IC50s = 422 and 1,607 ng/ml for D-6 and W-2 clones, respectively) and E. histolytica (IC50 = 82.7 μM).{45262,45263} Jatrorrhizine inhibits the growth of C8161 human melanoma cells in vitro (IC50 = 47.4 μM) and inhibits C8161 cell-mediated neovascularization in a Matrigel™ plug assay in mice when administered at a dose of 50 μg/animal.{45264} It reduces serum levels of triglycerides, LDL cholesterol (LDL-C), aspartate transaminase (AST), and alanine aminotransferase (ALT) in a high-fat diet-induced mouse model of hyperlipidemia when administered at doses of 20 and 100 mg/kg.{45265} Jatrorrhizine is also a metabolite of berberine (Item No. 10006427).{45266}  

     

    Brand:
    Cayman
    SKU:27314 - 1 mg

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  • Jatrorrhizine is an alkaloid that has been found in the Chinese herb C. chinensis and has diverse biological activities.{45262,45263,45264,45265} It is active against P. falciparum (IC50s = 422 and 1,607 ng/ml for D-6 and W-2 clones, respectively) and E. histolytica (IC50 = 82.7 μM).{45262,45263} Jatrorrhizine inhibits the growth of C8161 human melanoma cells in vitro (IC50 = 47.4 μM) and inhibits C8161 cell-mediated neovascularization in a Matrigel™ plug assay in mice when administered at a dose of 50 μg/animal.{45264} It reduces serum levels of triglycerides, LDL cholesterol (LDL-C), aspartate transaminase (AST), and alanine aminotransferase (ALT) in a high-fat diet-induced mouse model of hyperlipidemia when administered at doses of 20 and 100 mg/kg.{45265} Jatrorrhizine is also a metabolite of berberine (Item No. 10006427).{45266}  

     

    Brand:
    Cayman
    SKU:27314 - 10 mg

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  • Jatrorrhizine is an alkaloid that has been found in the Chinese herb C. chinensis and has diverse biological activities.{45262,45263,45264,45265} It is active against P. falciparum (IC50s = 422 and 1,607 ng/ml for D-6 and W-2 clones, respectively) and E. histolytica (IC50 = 82.7 μM).{45262,45263} Jatrorrhizine inhibits the growth of C8161 human melanoma cells in vitro (IC50 = 47.4 μM) and inhibits C8161 cell-mediated neovascularization in a Matrigel™ plug assay in mice when administered at a dose of 50 μg/animal.{45264} It reduces serum levels of triglycerides, LDL cholesterol (LDL-C), aspartate transaminase (AST), and alanine aminotransferase (ALT) in a high-fat diet-induced mouse model of hyperlipidemia when administered at doses of 20 and 100 mg/kg.{45265} Jatrorrhizine is also a metabolite of berberine (Item No. 10006427).{45266}  

     

    Brand:
    Cayman
    SKU:27314 - 5 mg

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  • JBIR-15 is a fungal metabolite produced by A. sclerotiorum.{40471} It has antifungal activity against C. albicans (MIC = 30 μM) but has no observable antibacterial activity against E. coli and S. aureus or cytotoxicity against HL-60 and A549 cells.  

     

    Brand:
    Cayman
    SKU:23860 - 1 mg

    Available on backorder

  • JBIR-15 is a fungal metabolite produced by A. sclerotiorum.{40471} It has antifungal activity against C. albicans (MIC = 30 μM) but has no observable antibacterial activity against E. coli and S. aureus or cytotoxicity against HL-60 and A549 cells.  

     

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    Cayman
    SKU:23860 - 250 µg

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  • JBSNF-000088 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50s = 1.8, 2.8, and 5 µM for human, monkey, and mouse NNMT, respectively).{50847} It inhibits NNMT and reduces 1-methyl-nicotinamide (MNA) levels in U2OS and 3T3L1 cells (IC50s = 1.6 and 6.3 µM, respectively). JBSNF-000088 (50 mg/kg) reduces visceral white adipose tissue (WAT) MNA levels, body weight, fed blood glucose levels, and plasma and liver triglyceride levels, and improves oral glucose tolerance in a mouse model of diet-induced obesity (DIO). It also improves glucose tolerance, without affecting body weight, in the ob/ob and db/db mouse models of insulin resistance and diabetes, respectively.  

     

    Brand:
    Cayman
    SKU:29920 - 1 g

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  • JBSNF-000088 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50s = 1.8, 2.8, and 5 µM for human, monkey, and mouse NNMT, respectively).{50847} It inhibits NNMT and reduces 1-methyl-nicotinamide (MNA) levels in U2OS and 3T3L1 cells (IC50s = 1.6 and 6.3 µM, respectively). JBSNF-000088 (50 mg/kg) reduces visceral white adipose tissue (WAT) MNA levels, body weight, fed blood glucose levels, and plasma and liver triglyceride levels, and improves oral glucose tolerance in a mouse model of diet-induced obesity (DIO). It also improves glucose tolerance, without affecting body weight, in the ob/ob and db/db mouse models of insulin resistance and diabetes, respectively.  

     

    Brand:
    Cayman
    SKU:29920 - 250 mg

    Available on backorder

  • JBSNF-000088 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50s = 1.8, 2.8, and 5 µM for human, monkey, and mouse NNMT, respectively).{50847} It inhibits NNMT and reduces 1-methyl-nicotinamide (MNA) levels in U2OS and 3T3L1 cells (IC50s = 1.6 and 6.3 µM, respectively). JBSNF-000088 (50 mg/kg) reduces visceral white adipose tissue (WAT) MNA levels, body weight, fed blood glucose levels, and plasma and liver triglyceride levels, and improves oral glucose tolerance in a mouse model of diet-induced obesity (DIO). It also improves glucose tolerance, without affecting body weight, in the ob/ob and db/db mouse models of insulin resistance and diabetes, respectively.  

     

    Brand:
    Cayman
    SKU:29920 - 500 mg

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  • JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis.{14421,14323,14322} It selectively enters mitochondria and changes fluorescence characteristics with alteration in mitochondrial transmembrane potential (ΔΨm). In healthy cells with a high mitochondrial ΔΨm, JC-1 forms complexes known as J-aggregates, which fluoresce red/orange and may be detected using FL2 settings by flow cytometry.{14322} A drop in ΔΨm, a very early event in apoptosis, results in JC-1 monomers, which fluoresce green (FL1 settings on flow cytometers).{14323,14322} JC-1 may also be used with fluorescent microscopes or plate readers, using excitation at 520-570 nm and emission at 570-610 nm for J-aggregates and excitation at 485 nm and emission at 535 nm for monomers.  

     

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    Cayman
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  • JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis.{14421,14323,14322} It selectively enters mitochondria and changes fluorescence characteristics with alteration in mitochondrial transmembrane potential (ΔΨm). In healthy cells with a high mitochondrial ΔΨm, JC-1 forms complexes known as J-aggregates, which fluoresce red/orange and may be detected using FL2 settings by flow cytometry.{14322} A drop in ΔΨm, a very early event in apoptosis, results in JC-1 monomers, which fluoresce green (FL1 settings on flow cytometers).{14323,14322} JC-1 may also be used with fluorescent microscopes or plate readers, using excitation at 520-570 nm and emission at 570-610 nm for J-aggregates and excitation at 485 nm and emission at 535 nm for monomers.  

     

    Brand:
    Cayman
    SKU:-
  • JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis.{14421,14323,14322} It selectively enters mitochondria and changes fluorescence characteristics with alteration in mitochondrial transmembrane potential (ΔΨm). In healthy cells with a high mitochondrial ΔΨm, JC-1 forms complexes known as J-aggregates, which fluoresce red/orange and may be detected using FL2 settings by flow cytometry.{14322} A drop in ΔΨm, a very early event in apoptosis, results in JC-1 monomers, which fluoresce green (FL1 settings on flow cytometers).{14323,14322} JC-1 may also be used with fluorescent microscopes or plate readers, using excitation at 520-570 nm and emission at 570-610 nm for J-aggregates and excitation at 485 nm and emission at 535 nm for monomers.  

     

    Brand:
    Cayman
    SKU:-
  • JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii.{46378} JCP174 enhances invasion of Toxoplasma tachyzoites into BSC-1 host cells, increasing the number of attached and invaded parasites when used at a concentration of 50 µM, enhancing plaque formation at concentrations of 0.5 and 50 µM, and increasing gliding motility. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase.{46379,46380}  

     

    Brand:
    Cayman
    SKU:21866 -

    Out of stock

  • JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii.{46378} JCP174 enhances invasion of Toxoplasma tachyzoites into BSC-1 host cells, increasing the number of attached and invaded parasites when used at a concentration of 50 µM, enhancing plaque formation at concentrations of 0.5 and 50 µM, and increasing gliding motility. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase.{46379,46380}  

     

    Brand:
    Cayman
    SKU:21866 -

    Out of stock

  • JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii.{46378} JCP174 enhances invasion of Toxoplasma tachyzoites into BSC-1 host cells, increasing the number of attached and invaded parasites when used at a concentration of 50 µM, enhancing plaque formation at concentrations of 0.5 and 50 µM, and increasing gliding motility. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase.{46379,46380}  

     

    Brand:
    Cayman
    SKU:21866 -

    Out of stock

  • JCP251 is a protease inhibitor.{46644} It inhibits neutrophil elastase when used at a concentration of 5 µM and reduces the activity of HIV protease and caspase-3 by 70 and 68%, respectively, when used at a concentration of 100 µM in cell-free assays.{46644,46645} JCP251 decreases amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) levels in HEK293 cells expressing wild-type and Swedish mutant amyloid precursor peptide (APP; IC50s = ~30 µM for both).{46646}  

     

    Brand:
    Cayman
    SKU:28712 - 10 mg

    Available on backorder

  • JCP251 is a protease inhibitor.{46644} It inhibits neutrophil elastase when used at a concentration of 5 µM and reduces the activity of HIV protease and caspase-3 by 70 and 68%, respectively, when used at a concentration of 100 µM in cell-free assays.{46644,46645} JCP251 decreases amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) levels in HEK293 cells expressing wild-type and Swedish mutant amyloid precursor peptide (APP; IC50s = ~30 µM for both).{46646}  

     

    Brand:
    Cayman
    SKU:28712 - 100 mg

    Available on backorder

  • JCP251 is a protease inhibitor.{46644} It inhibits neutrophil elastase when used at a concentration of 5 µM and reduces the activity of HIV protease and caspase-3 by 70 and 68%, respectively, when used at a concentration of 100 µM in cell-free assays.{46644,46645} JCP251 decreases amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) levels in HEK293 cells expressing wild-type and Swedish mutant amyloid precursor peptide (APP; IC50s = ~30 µM for both).{46646}  

     

    Brand:
    Cayman
    SKU:28712 - 250 mg

    Available on backorder

  • JCP251 is a protease inhibitor.{46644} It inhibits neutrophil elastase when used at a concentration of 5 µM and reduces the activity of HIV protease and caspase-3 by 70 and 68%, respectively, when used at a concentration of 100 µM in cell-free assays.{46644,46645} JCP251 decreases amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) levels in HEK293 cells expressing wild-type and Swedish mutant amyloid precursor peptide (APP; IC50s = ~30 µM for both).{46646}  

     

    Brand:
    Cayman
    SKU:28712 - 50 mg

    Available on backorder

  • Jervine is a naturally occurring teratogenic alkaloid that inhibits the sonic hedgehog pathway (IC50s = 500-700 nM) in vitro.{24330} It induces a variety of birth defects in vivo, including holoprosencephaly, cyclopia, cebocephaly, exencephaly, and microphthalmia in rat, chicken, and sheep.{35059,35060,35061} Jervine also reduces lipid accumulation and PPARγ and C/EBPα gene expression in 3T3-L1 adipocytes in vitro.{35062}  

     

    Brand:
    Cayman
    SKU:11723 - 1 mg

    Available on backorder

  • Jervine is a naturally occurring teratogenic alkaloid that inhibits the sonic hedgehog pathway (IC50s = 500-700 nM) in vitro.{24330} It induces a variety of birth defects in vivo, including holoprosencephaly, cyclopia, cebocephaly, exencephaly, and microphthalmia in rat, chicken, and sheep.{35059,35060,35061} Jervine also reduces lipid accumulation and PPARγ and C/EBPα gene expression in 3T3-L1 adipocytes in vitro.{35062}  

     

    Brand:
    Cayman
    SKU:11723 - 10 mg

    Available on backorder

  • Jervine is a naturally occurring teratogenic alkaloid that inhibits the sonic hedgehog pathway (IC50s = 500-700 nM) in vitro.{24330} It induces a variety of birth defects in vivo, including holoprosencephaly, cyclopia, cebocephaly, exencephaly, and microphthalmia in rat, chicken, and sheep.{35059,35060,35061} Jervine also reduces lipid accumulation and PPARγ and C/EBPα gene expression in 3T3-L1 adipocytes in vitro.{35062}  

     

    Brand:
    Cayman
    SKU:11723 - 5 mg

    Available on backorder

  • Jervine is a naturally occurring teratogenic alkaloid that inhibits the sonic hedgehog pathway (IC50s = 500-700 nM) in vitro.{24330} It induces a variety of birth defects in vivo, including holoprosencephaly, cyclopia, cebocephaly, exencephaly, and microphthalmia in rat, chicken, and sheep.{35059,35060,35061} Jervine also reduces lipid accumulation and PPARγ and C/EBPα gene expression in 3T3-L1 adipocytes in vitro.{35062}  

     

    Brand:
    Cayman
    SKU:11723 - 50 mg

    Available on backorder

  • Human sirtuin 2 (SIRT2) is a NAD+-dependent protein deacetylase with diverse targets, including α-tubulin, phosphoenolpyruvate carboxykinase, and forkhead box protein O1. JFD00244 is an inhibitor of SIRT2 (IC50= 56.7 µM).{23576} At 5 µM, JFD00244 induces granulocytic differentiation in the acute promyelocytic leukemia cell line NB4.{23577}  

     

    Brand:
    Cayman
    SKU:-
  • Human sirtuin 2 (SIRT2) is a NAD+-dependent protein deacetylase with diverse targets, including α-tubulin, phosphoenolpyruvate carboxykinase, and forkhead box protein O1. JFD00244 is an inhibitor of SIRT2 (IC50= 56.7 µM).{23576} At 5 µM, JFD00244 induces granulocytic differentiation in the acute promyelocytic leukemia cell line NB4.{23577}  

     

    Brand:
    Cayman
    SKU:-
  • Human sirtuin 2 (SIRT2) is a NAD+-dependent protein deacetylase with diverse targets, including α-tubulin, phosphoenolpyruvate carboxykinase, and forkhead box protein O1. JFD00244 is an inhibitor of SIRT2 (IC50= 56.7 µM).{23576} At 5 µM, JFD00244 induces granulocytic differentiation in the acute promyelocytic leukemia cell line NB4.{23577}  

     

    Brand:
    Cayman
    SKU:-
  • The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.  

     

    Brand:
    Cayman
    SKU:10641 - 1 mg

    Available on backorder

  • The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.  

     

    Brand:
    Cayman
    SKU:10641 - 10 mg

    Available on backorder

  • The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.  

     

    Brand:
    Cayman
    SKU:10641 - 25 mg

    Available on backorder

  • The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis.{15106,16291} JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay.{18667} It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.  

     

    Brand:
    Cayman
    SKU:10641 - 5 mg

    Available on backorder

  • JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:22905 - 1 mg

    Available on backorder

  • JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:22905 - 10 mg

    Available on backorder

  • JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:22905 - 25 mg

    Available on backorder

  • JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.  

     

    Brand:
    Cayman
    SKU:22905 - 5 mg

    Available on backorder

  • JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}  

     

    Brand:
    Cayman
    SKU:-
  • JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}  

     

    Brand:
    Cayman
    SKU:-
  • JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}  

     

    Brand:
    Cayman
    SKU:-
  • JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}  

     

    Brand:
    Cayman
    SKU:-
  • JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA (Item No. 17037) with an IC50 value of 0.57 µM.{30849} JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2.{30849} JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.{30849}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}  

     

    Brand:
    Cayman
    SKU:-
  • JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}  

     

    Brand:
    Cayman
    SKU:-
  • JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}  

     

    Brand:
    Cayman
    SKU:-
  • JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM).{24518} It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function.{24518,24517} JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).{24518}  

     

    Brand:
    Cayman
    SKU:-
  • JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1674 reduces viability of LOX-IMVI cancer cells (EC50 = 0.03 µM) and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30784 - 1 mg

    Available on backorder

  • JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1674 reduces viability of LOX-IMVI cancer cells (EC50 = 0.03 µM) and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30784 - 5 mg

    Available on backorder

  • JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30786 - 1 mg

    Available on backorder

  • JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30786 - 10 mg

    Available on backorder

  • JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30786 - 25 mg

    Available on backorder

  • JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 (Item No. 23282).{55163} JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).  

     

    Brand:
    Cayman
    SKU:30786 - 5 mg

    Available on backorder

  • Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}  

     

    Brand:
    Cayman
    SKU:10012699 - 1 mg

    Available on backorder

  • Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}  

     

    Brand:
    Cayman
    SKU:10012699 - 100 µg

    Available on backorder

  • Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}  

     

    Brand:
    Cayman
    SKU:10012699 - 5 mg

    Available on backorder

  • Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro.{15848} At 80 µg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats.{15848} JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 µg/kg.{15848}  

     

    Brand:
    Cayman
    SKU:10012699 - 500 µg

    Available on backorder

  • JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:31781 - 1 mg

    Available on backorder

  • JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:31781 - 10 mg

    Available on backorder

  • JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:31781 - 25 mg

    Available on backorder

  • JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:31781 - 5 mg

    Available on backorder

  • JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}  

     

    Brand:
    Cayman
    SKU:11997 - 1 mg

    Available on backorder

  • JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}  

     

    Brand:
    Cayman
    SKU:11997 - 5 mg

    Available on backorder

  • JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}  

     

    Brand:
    Cayman
    SKU:11997 - 500 µg

    Available on backorder

  • Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.  

     

    Brand:
    Cayman
    SKU:10008131 - 1 mg

    Available on backorder

  • Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.  

     

    Brand:
    Cayman
    SKU:10008131 - 10 mg

    Available on backorder

  • Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.  

     

    Brand:
    Cayman
    SKU:10008131 - 5 mg

    Available on backorder

  • Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.{14399} JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.{13764} JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.  

     

    Brand:
    Cayman
    SKU:10008131 - 50 mg

    Available on backorder

  • JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}  

     

    Brand:
    Cayman
    SKU:-
  • JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}  

     

    Brand:
    Cayman
    SKU:-
  • JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).{26505,26508,26507} It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.{26505} Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.{26505} This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.{26506}  

     

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  • Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}  

     

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    Cayman
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  • Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}  

     

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    Cayman
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  • Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}  

     

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    Cayman
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  • Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines, including the endocannabinoid arachidonoyl ethanolamide (AEA). JNJ-1661010 is a selective inhibitor of FAAH (IC50s = 34 and 33 nM in rat and human, respectively) that is able to cross the blood-brain barrier.{22625} At 20 mg/kg, JNJ-1661010 has been shown to elevate levels of AEA in rat brain.{22625} This compound has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.{22644}  

     

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    Cayman
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  • JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}  

     

    Brand:
    Cayman
    SKU:30930 - 10 mg

    Available on backorder

  • JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}  

     

    Brand:
    Cayman
    SKU:30930 - 25 mg

    Available on backorder

  • JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}  

     

    Brand:
    Cayman
    SKU:30930 - 5 mg

    Available on backorder

  • JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}  

     

    Brand:
    Cayman
    SKU:30930 - 50 mg

    Available on backorder

  • JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}  

     

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    Cayman
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  • JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}  

     

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    Cayman
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  • JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}  

     

    Brand:
    Cayman
    SKU:-
  • JNJ-26481585 is a hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50 = 0.11 nM).{32219} For other HDACs, IC50 values range from 0.33, 0.37, and 0.46 nM for HDACs 2, 11, and 10, respectively, to 32, 77, and 119 nM for HDACs 9, 6, and 7, respectively.{32219} JNJ-26481585 induces apoptosis and cell cycle arrest in multiple myeloma cells and complete tumor growth inhibition in Ras mutant HCT116 colon carcinoma or multiple myeloma xenografts.{32219,32220}  

     

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    Cayman
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  • The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}  

     

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    Cayman
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  • The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}  

     

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    Cayman
    SKU:-
  • The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}  

     

    Brand:
    Cayman
    SKU:-
  • The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}  

     

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    Cayman
    SKU:-
  • JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}  

     

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    Cayman
    SKU:-

    Available on backorder

  • JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}  

     

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    Cayman
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    Available on backorder

  • JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}  

     

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    Cayman
    SKU:-

    Available on backorder

  • JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.{38509,38510} JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).{38509} Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.{38511} It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.{38512} In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.{38515}  

     

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    Cayman
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  • JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}  

     

    Brand:
    Cayman
    SKU:27650 - 10 mg

    Available on backorder

  • JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}  

     

    Brand:
    Cayman
    SKU:27650 - 100 mg

    Available on backorder

  • JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}  

     

    Brand:
    Cayman
    SKU:27650 - 5 mg

    Available on backorder

  • JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}  

     

    Brand:
    Cayman
    SKU:27650 - 50 mg

    Available on backorder

  • JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.  

     

    Brand:
    Cayman
    SKU:21869 -

    Out of stock

  • JNJ-40418677 is a modulator of γ-secretase.{46387} It reduces the levels of amyloid-β (1-42) (Aβ42; Item No. 20574) in a cell-free γ-secretase modulation assay. It also reduces the secretion of Aβ42, but not total Aβ, in SK-N-BE(2) human neuroblastoma cells expressing amyloid precursor protein (APP; mean IC50 = 200 nM) and in primary rat cortical neurons (mean IC50 = 185 nM). JNJ-40418677 (100 and 300 mg/kg) reduces the level of Aβ42 in wild-type mouse brain. It decreases brain levels of Aβ42, Aβ40, and Aβ38 in the deposited fraction, and Aβ42 and Aβ40 in the soluble fraction, in the Tg2576 mouse model of Alzheimer’s disease when administered at doses of 60 and 120 mg/kg per day in the diet for seven months. It also reduces increases in the number of amyloid plaques in Tg2576 mouse brain compared to vehicle control animals.  

     

    Brand:
    Cayman
    SKU:21869 -

    Out of stock