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Showing 43201–43350 of 45550 results

  • Ubiquitin is a small protein that occurs in all eukaryotic cells. The ubiquitin protein itself consists of 76 amino acids and has a molecular mass of about 8.5 kDa. Key features include its C-terminal tail and the 7 Lys residues. It is highly conserved among eukaryotic species: human and yeast ubiquitin share 96% sequence identity.{17707} The main function of ubiquitin is to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome.{17708} Ubiquitination represents an essential cellular process affected by a multi-enzyme cascade involving classes of enzymes known as ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s or Ubcs) and ubiquitin-protein ligases (E3s). Ubiquitin is activated in a two-step reaction by an E1 ubiquitin-activating enzyme in a process requiring ATP as an energy source. The initial step involves production of a ubiquitin-adenylate intermediate. The second step transfers ubiquitin to the E1 active site cysteine residue, with release of AMP. This step results in a thioester linkage between the C-terminal carboxyl group of ubiquitin and the E1 cysteine sulfhydryl group. The third step is a transfer of ubiquitin from E1 to the active site cysteine of a ubiquitin-conjugating enzyme E2 via a trans(thio)esterification reaction. And the final step of the ubiquitylation cascade creates an isopeptide bond between a lysine of the target protein and the C-terminal glycine of ubiquitin. In general, this step requires the activity of one of the hundreds of E3 ubiquitin-protein ligases (often termed simply ubiquitin ligase). E3 enzymes function as the substrate recognition modules of the system and are capable of interaction with both E2 and substrate.{17708,17709} Ubiquitination also participates in the internalization and degradation of plasma membrane proteins such as some of the TCR subunits while still ER-membrane associated.{17712} Ubiquitin also plays a role in regulating signal transduction cascades through the elimination inhibitor proteins, such as IκBα and p27.{17713}  

     

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    SKU:13724 - 200 µg

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  • Antigen: native bovine ubiquitin conjugated to KLH • Host: rabbit • Cross Reactivity: (+) human, monkey, mouse, rat, hamster, rabbit, guinea pig, bovine, porcine, canine, pvine, chicken, Xenopus, yeast, Drosophila, and Rainbow Trout ubiquitin • Application(s): WB, IP, and ChIP • Ubiquitin functions to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome. The ubiquitination process participates in the internalization and degradation of plasma membrane proteins and also plays a role in regulating signal transduction cascades through the elimination of inhibitor proteins.  

     

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    SKU:13724- 200 µg

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  • Antigen: native bovine ubiquitin conjugated to KLH • Host: rabbit • Cross Reactivity: (+) human, monkey, mouse, rat, hamster, rabbit, guinea pig, bovine, porcine, canine, pvine, chicken, Xenopus, yeast, Drosophila, and Rainbow Trout ubiquitin • Application(s): WB, IP, and ChIP • Ubiquitin functions to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome. The ubiquitination process participates in the internalization and degradation of plasma membrane proteins and also plays a role in regulating signal transduction cascades through the elimination of inhibitor proteins.  

     

    Brand:
    Cayman
    SKU:13724- 200 µg
  • Ubiquitin is a small protein that occurs in all eukaryotic cells. The ubiquitin protein itself consists of 76 amino acids and has a molecular mass of about 8.5 kDa. Key features include its C-terminal tail and the 7 Lys residues. It is highly conserved among eukaryotic species: human and yeast ubiquitin share 96% sequence identity.{17707} The main function of ubiquitin is to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome.{17708} Ubiquitination represents an essential cellular process affected by a multi-enzyme cascade involving classes of enzymes known as ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s or Ubcs) and ubiquitin-protein ligases (E3s). Ubiquitin is activated in a two-step reaction by an E1 ubiquitin-activating enzyme in a process requiring ATP as an energy source. The initial step involves production of a ubiquitin-adenylate intermediate. The second step transfers ubiquitin to the E1 active site cysteine residue, with release of AMP. This step results in a thioester linkage between the C-terminal carboxyl group of ubiquitin and the E1 cysteine sulfhydryl group. The third step is a transfer of ubiquitin from E1 to the active site cysteine of a ubiquitin-conjugating enzyme E2 via a trans(thio)esterification reaction. And the final step of the ubiquitylation cascade creates an isopeptide bond between a lysine of the target protein and the C-terminal glycine of ubiquitin. In general, this step requires the activity of one of the hundreds of E3 ubiquitin-protein ligases (often termed simply ubiquitin ligase). E3 enzymes function as the substrate recognition modules of the system and are capable of interaction with both E2 and substrate.{17708,17709} Ubiquitination also participates in the internalization and degradation of plasma membrane proteins such as some of the TCR subunits while still ER-membrane associated.{17712} Ubiquitin also plays a role in regulating signal transduction cascades through the elimination inhibitor proteins, such as IκBα and p27.{17713}  

     

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    SKU:13724 - 50 µg

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  • Antigen: native bovine ubiquitin conjugated to KLH • Host: rabbit • Cross Reactivity: (+) human, monkey, mouse, rat, hamster, rabbit, guinea pig, bovine, porcine, canine, pvine, chicken, Xenopus, yeast, Drosophila, and Rainbow Trout ubiquitin • Application(s): WB, IP, and ChIP • Ubiquitin functions to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome. The ubiquitination process participates in the internalization and degradation of plasma membrane proteins and also plays a role in regulating signal transduction cascades through the elimination of inhibitor proteins.  

     

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    SKU:13724- 50 µg

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  • Antigen: native bovine ubiquitin conjugated to KLH • Host: rabbit • Cross Reactivity: (+) human, monkey, mouse, rat, hamster, rabbit, guinea pig, bovine, porcine, canine, pvine, chicken, Xenopus, yeast, Drosophila, and Rainbow Trout ubiquitin • Application(s): WB, IP, and ChIP • Ubiquitin functions to clear abnormal, foreign and improperly folded proteins by targeting them for degradation by the 26S proteasome. The ubiquitination process participates in the internalization and degradation of plasma membrane proteins and also plays a role in regulating signal transduction cascades through the elimination of inhibitor proteins.  

     

    Brand:
    Cayman
    SKU:13724- 50 µg
  • UBP 301 is an antagonist of the kainate receptor, an ionotropic glutamate receptor (apparent Kd = 5.94 µM).{28499} It displays ~30-fold selectivity over AMPA receptors.{28499} UBP 301 is used to assess the roles of kainate receptors in neuronal signaling, particularly in reference to neuropathic pain.{28501,28500}  

     

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  • UBP 301 is an antagonist of the kainate receptor, an ionotropic glutamate receptor (apparent Kd = 5.94 µM).{28499} It displays ~30-fold selectivity over AMPA receptors.{28499} UBP 301 is used to assess the roles of kainate receptors in neuronal signaling, particularly in reference to neuropathic pain.{28501,28500}  

     

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  • UBP 301 is an antagonist of the kainate receptor, an ionotropic glutamate receptor (apparent Kd = 5.94 µM).{28499} It displays ~30-fold selectivity over AMPA receptors.{28499} UBP 301 is used to assess the roles of kainate receptors in neuronal signaling, particularly in reference to neuropathic pain.{28501,28500}  

     

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  • UBP 302 is an antagonist of glutamate receptor 5 (GluR5) subunit-containing kainate receptors that inhibits kainate-induced responses in isolated rat dorsal roots (Kd = 402 nM).{38631} In vitro, UBP 302 inhibits gamma frequency oscillations in the rat basolateral amygdala at a concentration of 25 µM, and blocks kainate receptor signaling in layer III neurons within the mouse medial entorhinal cortex at 20 µM, abrogating the intense synaptic activity characteristic of the Up state of cortical slow oscillation.{38629,38628} In vivo, UBP 302 (250 mg/kg) significantly reduces seizure severity in a rat model of soman-induced status epilepticus.{38630}  

     

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    Cayman
    SKU:24309 - 1 mg

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  • UBP 302 is an antagonist of glutamate receptor 5 (GluR5) subunit-containing kainate receptors that inhibits kainate-induced responses in isolated rat dorsal roots (Kd = 402 nM).{38631} In vitro, UBP 302 inhibits gamma frequency oscillations in the rat basolateral amygdala at a concentration of 25 µM, and blocks kainate receptor signaling in layer III neurons within the mouse medial entorhinal cortex at 20 µM, abrogating the intense synaptic activity characteristic of the Up state of cortical slow oscillation.{38629,38628} In vivo, UBP 302 (250 mg/kg) significantly reduces seizure severity in a rat model of soman-induced status epilepticus.{38630}  

     

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    SKU:24309 - 5 mg

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  • UBP 310 is an antagonist of ionotropic glutamate receptor 5 (GluR5 or GluK1; Kd = 130 nM).{34458,34460,34461} It less potently binds GluR2 (GluA2) and GluR6 (GluK2; Kds = 106 and 1,626 µM, respectively).{34459,34460} UBP 310 is inactive at metabotropic GluR group I and NMDA receptors.  

     

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    SKU:21806 -

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  • UBP 310 is an antagonist of ionotropic glutamate receptor 5 (GluR5 or GluK1; Kd = 130 nM).{34458,34460,34461} It less potently binds GluR2 (GluA2) and GluR6 (GluK2; Kds = 106 and 1,626 µM, respectively).{34459,34460} UBP 310 is inactive at metabotropic GluR group I and NMDA receptors.  

     

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    SKU:21806 -

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  • UBP 310 is an antagonist of ionotropic glutamate receptor 5 (GluR5 or GluK1; Kd = 130 nM).{34458,34460,34461} It less potently binds GluR2 (GluA2) and GluR6 (GluK2; Kds = 106 and 1,626 µM, respectively).{34459,34460} UBP 310 is inactive at metabotropic GluR group I and NMDA receptors.  

     

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    SKU:21806 -

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  • Mammalian Omi/HtrA2 is a serine protease localized in mitochondria with close homology to bacterial HtrA chaperones. It is released from the mitochondria in response to apoptotic stimuli whereupon it induces cell death through both a caspase-dependent manner and a mechanism that involves its protease activity. UCF 101 is an inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM).{25354} It is highly specific for Omi/HtrA2, demonstrating less potent activity when tested against a panel of various other serine proteases (IC50s range from 200 to >500 μM).{25354} Additionally, UCF 101 is naturally fluorescent, thus enabling the visualization of its entry into cells.{25354} UCF 101 has been used to decrease cerebral infarct size in a rat model of cerebral ischemia, demonstrating neuroprotective effects by reducing apoptosis of cortical cells.{25355} It has also been reported to be protective of cardiomyocytes against ischemic injury through a mechanism that prevents Omi/HtrA2 proteolysis of Thanatos-associated protein 5, a cardiac-specific nuclear protein that controls cell cycle progression.{25356}  

     

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  • Mammalian Omi/HtrA2 is a serine protease localized in mitochondria with close homology to bacterial HtrA chaperones. It is released from the mitochondria in response to apoptotic stimuli whereupon it induces cell death through both a caspase-dependent manner and a mechanism that involves its protease activity. UCF 101 is an inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM).{25354} It is highly specific for Omi/HtrA2, demonstrating less potent activity when tested against a panel of various other serine proteases (IC50s range from 200 to >500 μM).{25354} Additionally, UCF 101 is naturally fluorescent, thus enabling the visualization of its entry into cells.{25354} UCF 101 has been used to decrease cerebral infarct size in a rat model of cerebral ischemia, demonstrating neuroprotective effects by reducing apoptosis of cortical cells.{25355} It has also been reported to be protective of cardiomyocytes against ischemic injury through a mechanism that prevents Omi/HtrA2 proteolysis of Thanatos-associated protein 5, a cardiac-specific nuclear protein that controls cell cycle progression.{25356}  

     

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  • Mammalian Omi/HtrA2 is a serine protease localized in mitochondria with close homology to bacterial HtrA chaperones. It is released from the mitochondria in response to apoptotic stimuli whereupon it induces cell death through both a caspase-dependent manner and a mechanism that involves its protease activity. UCF 101 is an inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM).{25354} It is highly specific for Omi/HtrA2, demonstrating less potent activity when tested against a panel of various other serine proteases (IC50s range from 200 to >500 μM).{25354} Additionally, UCF 101 is naturally fluorescent, thus enabling the visualization of its entry into cells.{25354} UCF 101 has been used to decrease cerebral infarct size in a rat model of cerebral ischemia, demonstrating neuroprotective effects by reducing apoptosis of cortical cells.{25355} It has also been reported to be protective of cardiomyocytes against ischemic injury through a mechanism that prevents Omi/HtrA2 proteolysis of Thanatos-associated protein 5, a cardiac-specific nuclear protein that controls cell cycle progression.{25356}  

     

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  • Mammalian Omi/HtrA2 is a serine protease localized in mitochondria with close homology to bacterial HtrA chaperones. It is released from the mitochondria in response to apoptotic stimuli whereupon it induces cell death through both a caspase-dependent manner and a mechanism that involves its protease activity. UCF 101 is an inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM).{25354} It is highly specific for Omi/HtrA2, demonstrating less potent activity when tested against a panel of various other serine proteases (IC50s range from 200 to >500 μM).{25354} Additionally, UCF 101 is naturally fluorescent, thus enabling the visualization of its entry into cells.{25354} UCF 101 has been used to decrease cerebral infarct size in a rat model of cerebral ischemia, demonstrating neuroprotective effects by reducing apoptosis of cortical cells.{25355} It has also been reported to be protective of cardiomyocytes against ischemic injury through a mechanism that prevents Omi/HtrA2 proteolysis of Thanatos-associated protein 5, a cardiac-specific nuclear protein that controls cell cycle progression.{25356}  

     

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  • UCM05 is an inhibitor of fatty acid synthase that strongly suppresses the growth of human breast cancer cell lines (IC50 = 21 µM for SK-BR-3 cells).{30886,30889} It does not alter carnitine palmitoyltransferase 1 activity or induce weight loss in mice.{30886,30889} UCM05 can reduce cleavage of poly(ADP-ribose) polymerase, phosphorylation of HER2, Akt, and ERK1/2, and growth of established xenografts in vivo.{30887} UCM05 also blocks the GTP-binding site of the cell division protein FtsZ from Bacillus, preventing bacterial division.{30888}  

     

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  • UCM05 is an inhibitor of fatty acid synthase that strongly suppresses the growth of human breast cancer cell lines (IC50 = 21 µM for SK-BR-3 cells).{30886,30889} It does not alter carnitine palmitoyltransferase 1 activity or induce weight loss in mice.{30886,30889} UCM05 can reduce cleavage of poly(ADP-ribose) polymerase, phosphorylation of HER2, Akt, and ERK1/2, and growth of established xenografts in vivo.{30887} UCM05 also blocks the GTP-binding site of the cell division protein FtsZ from Bacillus, preventing bacterial division.{30888}  

     

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  • UCM05 is an inhibitor of fatty acid synthase that strongly suppresses the growth of human breast cancer cell lines (IC50 = 21 µM for SK-BR-3 cells).{30886,30889} It does not alter carnitine palmitoyltransferase 1 activity or induce weight loss in mice.{30886,30889} UCM05 can reduce cleavage of poly(ADP-ribose) polymerase, phosphorylation of HER2, Akt, and ERK1/2, and growth of established xenografts in vivo.{30887} UCM05 also blocks the GTP-binding site of the cell division protein FtsZ from Bacillus, preventing bacterial division.{30888}  

     

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  • Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide) potentiate its biological activity.{1134} This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons.{10647} One of the more potent and selective reuptake inhibitors is UCM707, a 3-furyl arachidonoyl analog. UCM707 has an IC50 of 0.8 µM for the inhibition of tritiated AEA uptake into human U937 cells but has low affinity for FAAH, exhibiting an IC50 value of 30 µM.{11303} UCM707 also potentiates the biological effects of AEA when co-administered in rats.{10504}  

     

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    SKU:10045 - 10 mg

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  • Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide) potentiate its biological activity.{1134} This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons.{10647} One of the more potent and selective reuptake inhibitors is UCM707, a 3-furyl arachidonoyl analog. UCM707 has an IC50 of 0.8 µM for the inhibition of tritiated AEA uptake into human U937 cells but has low affinity for FAAH, exhibiting an IC50 value of 30 µM.{11303} UCM707 also potentiates the biological effects of AEA when co-administered in rats.{10504}  

     

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    SKU:10045 - 25 mg

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  • Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide) potentiate its biological activity.{1134} This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons.{10647} One of the more potent and selective reuptake inhibitors is UCM707, a 3-furyl arachidonoyl analog. UCM707 has an IC50 of 0.8 µM for the inhibition of tritiated AEA uptake into human U937 cells but has low affinity for FAAH, exhibiting an IC50 value of 30 µM.{11303} UCM707 also potentiates the biological effects of AEA when co-administered in rats.{10504}  

     

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    Cayman
    SKU:10045 - 5 mg

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  • Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide) potentiate its biological activity.{1134} This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons.{10647} One of the more potent and selective reuptake inhibitors is UCM707, a 3-furyl arachidonoyl analog. UCM707 has an IC50 of 0.8 µM for the inhibition of tritiated AEA uptake into human U937 cells but has low affinity for FAAH, exhibiting an IC50 value of 30 µM.{11303} UCM707 also potentiates the biological effects of AEA when co-administered in rats.{10504}  

     

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    SKU:10045 - 50 mg

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  • UCN-01 is a synthetic derivative of staurosporine (Item No. 81590) with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM) and cyclin-dependent kinases (IC50s = 300-600 nM for Cdk1 and Cdk2).{24026,24210,23163} UCN-01 arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase Chk1 (IC50 = 7 nM), leading to apoptosis.{24026,29273,29274,29272}  

     

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  • UCN-02 is a derivative of staurosporine (Item No. 81590) and a stereoisomer of UCN-01 (Item No. 18130) first isolated from a high staurosporine-producing Streptomyces culture as a minor co-metabolite.{31858} UCN-02 inhibits protein kinase C with a slightly reduced potency than UCN-01 (IC50 = 62 and 4.1 nM, for UNC-02 and UCN-01, respectively) and is cytotoxic to the growth of HeLa S3 cells.{31858}  

     

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    SKU:20221 -

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  • UCN-02 is a derivative of staurosporine (Item No. 81590) and a stereoisomer of UCN-01 (Item No. 18130) first isolated from a high staurosporine-producing Streptomyces culture as a minor co-metabolite.{31858} UCN-02 inhibits protein kinase C with a slightly reduced potency than UCN-01 (IC50 = 62 and 4.1 nM, for UNC-02 and UCN-01, respectively) and is cytotoxic to the growth of HeLa S3 cells.{31858}  

     

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    SKU:20221 -

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  • UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system.{40197,40196} UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 µM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter.{40198} It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 µM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 µM.{40196} UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.{40197}  

     

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    SKU:21460 -

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  • UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system.{40197,40196} UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 µM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter.{40198} It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 µM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 µM.{40196} UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.{40197}  

     

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    SKU:21460 -

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  • UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system.{40197,40196} UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 µM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter.{40198} It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 µM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 µM.{40196} UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.{40197}  

     

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    SKU:21460 -

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  • Udenafil is an inhibitor of phosphodiesterase 5 (PDE5).{56058,56059,56060} In vivo, udenafil (1 and 5 mg/kg) increases lung cGMP levels, attenuates the development of compensatory right ventricular hypertrophy, and reduces pulmonary arterial wall thickening in a rat model of monocrotaline-induced pulmonary hypertension.{56058} It increases creatine clearance and decreases blood urea nitrogen (BUN) and serum malondialdehyde (MDA) levels in a rat model of renal ischemia-reperfusion injury.{56059} Udenafil (0.3 and 10 mg/kg) induces penile erections in conscious rabbits and in rabbits with acute spinal cord injury.{56060}  

     

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    SKU:30373 - 10 mg

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  • Udenafil is an inhibitor of phosphodiesterase 5 (PDE5).{56058,56059,56060} In vivo, udenafil (1 and 5 mg/kg) increases lung cGMP levels, attenuates the development of compensatory right ventricular hypertrophy, and reduces pulmonary arterial wall thickening in a rat model of monocrotaline-induced pulmonary hypertension.{56058} It increases creatine clearance and decreases blood urea nitrogen (BUN) and serum malondialdehyde (MDA) levels in a rat model of renal ischemia-reperfusion injury.{56059} Udenafil (0.3 and 10 mg/kg) induces penile erections in conscious rabbits and in rabbits with acute spinal cord injury.{56060}  

     

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    SKU:30373 - 25 mg

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  • Udenafil is an inhibitor of phosphodiesterase 5 (PDE5).{56058,56059,56060} In vivo, udenafil (1 and 5 mg/kg) increases lung cGMP levels, attenuates the development of compensatory right ventricular hypertrophy, and reduces pulmonary arterial wall thickening in a rat model of monocrotaline-induced pulmonary hypertension.{56058} It increases creatine clearance and decreases blood urea nitrogen (BUN) and serum malondialdehyde (MDA) levels in a rat model of renal ischemia-reperfusion injury.{56059} Udenafil (0.3 and 10 mg/kg) induces penile erections in conscious rabbits and in rabbits with acute spinal cord injury.{56060}  

     

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    SKU:30373 - 5 mg

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  • Udenafil is an inhibitor of phosphodiesterase 5 (PDE5).{56058,56059,56060} In vivo, udenafil (1 and 5 mg/kg) increases lung cGMP levels, attenuates the development of compensatory right ventricular hypertrophy, and reduces pulmonary arterial wall thickening in a rat model of monocrotaline-induced pulmonary hypertension.{56058} It increases creatine clearance and decreases blood urea nitrogen (BUN) and serum malondialdehyde (MDA) levels in a rat model of renal ischemia-reperfusion injury.{56059} Udenafil (0.3 and 10 mg/kg) induces penile erections in conscious rabbits and in rabbits with acute spinal cord injury.{56060}  

     

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    SKU:30373 - 50 mg

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  • UDP is the diphosphate of the nucleoside uridine. It is a specific agonist of the P2Y purinoceptor P2Y6 (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction.{23976,27687,29424,29425,29423,29426} UDP also acts as an antagonist of P2Y14, whose agonists include UDP-glucose (Item No. 15602), UDP-galactose, and UDP-glucuronic acid.{23976,27687}  

     

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  • UDP is the diphosphate of the nucleoside uridine. It is a specific agonist of the P2Y purinoceptor P2Y6 (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction.{23976,27687,29424,29425,29423,29426} UDP also acts as an antagonist of P2Y14, whose agonists include UDP-glucose (Item No. 15602), UDP-galactose, and UDP-glucuronic acid.{23976,27687}  

     

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  • UDP is the diphosphate of the nucleoside uridine. It is a specific agonist of the P2Y purinoceptor P2Y6 (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction.{23976,27687,29424,29425,29423,29426} UDP also acts as an antagonist of P2Y14, whose agonists include UDP-glucose (Item No. 15602), UDP-galactose, and UDP-glucuronic acid.{23976,27687}  

     

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  • UDP-N-acetyl-D-Glucosamine is a natural nucleotide sugar that is used by glycosyltransferases to transfer N-acetyl-D-glucosamine (Item No. 13136) residues to substrates.{38008} It is an important component of antibiotic biosynthesis pathways in fungi and lipopolysaccharide production in bacteria.{38006,38007}  

     

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    SKU:20353 -

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  • UDP-N-acetyl-D-Glucosamine is a natural nucleotide sugar that is used by glycosyltransferases to transfer N-acetyl-D-glucosamine (Item No. 13136) residues to substrates.{38008} It is an important component of antibiotic biosynthesis pathways in fungi and lipopolysaccharide production in bacteria.{38006,38007}  

     

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    SKU:20353 -

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  • UDP-N-acetyl-D-Glucosamine is a natural nucleotide sugar that is used by glycosyltransferases to transfer N-acetyl-D-glucosamine (Item No. 13136) residues to substrates.{38008} It is an important component of antibiotic biosynthesis pathways in fungi and lipopolysaccharide production in bacteria.{38006,38007}  

     

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    SKU:20353 -

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  • UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14 receptor (EC50 = 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.{23976} It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.{16468}  

     

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  • UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14 receptor (EC50 = 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.{23976} It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.{16468}  

     

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  • UDP-β-D-Glucose is the stereoisomer of UDP-α-D-glucose (sodium salt) (Item No. 15602). The activities of the UDP-β-D-glucose isomer are not known.  

     

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    Cayman
    SKU:21620 -

    Out of stock

  • UDP-β-D-Glucose is the stereoisomer of UDP-α-D-glucose (sodium salt) (Item No. 15602). The activities of the UDP-β-D-glucose isomer are not known.  

     

    Brand:
    Cayman
    SKU:21620 -

    Out of stock

  • UDP-β-D-Glucose is the stereoisomer of UDP-α-D-glucose (sodium salt) (Item No. 15602). The activities of the UDP-β-D-glucose isomer are not known.  

     

    Brand:
    Cayman
    SKU:21620 -

    Out of stock

  • UDP-β-D-Glucose is the stereoisomer of UDP-α-D-glucose (sodium salt) (Item No. 15602). The activities of the UDP-β-D-glucose isomer are not known.  

     

    Brand:
    Cayman
    SKU:21620 -

    Out of stock

  • UF010 is a class I HDAC inhibitor with IC50 values of 0.06, 0.1, 0.5, and 1.5 µM for HDAC3, 2, 1, and 8, respectively.{33362} It is more than 6-fold selective for these class I HDACs over any additional HDACs.{33362} UF010 is reported to inhibit cancer cell proliferation with a mean GI50 value of 2.94 μM when screened against the NCI-60 panel of cancer cell lines and functions by blocking the G1/S phase of the cell cycle.{33362}  

     

    Brand:
    Cayman
    SKU:21273 -

    Out of stock

  • UF010 is a class I HDAC inhibitor with IC50 values of 0.06, 0.1, 0.5, and 1.5 µM for HDAC3, 2, 1, and 8, respectively.{33362} It is more than 6-fold selective for these class I HDACs over any additional HDACs.{33362} UF010 is reported to inhibit cancer cell proliferation with a mean GI50 value of 2.94 μM when screened against the NCI-60 panel of cancer cell lines and functions by blocking the G1/S phase of the cell cycle.{33362}  

     

    Brand:
    Cayman
    SKU:21273 -

    Out of stock

  • UF010 is a class I HDAC inhibitor with IC50 values of 0.06, 0.1, 0.5, and 1.5 µM for HDAC3, 2, 1, and 8, respectively.{33362} It is more than 6-fold selective for these class I HDACs over any additional HDACs.{33362} UF010 is reported to inhibit cancer cell proliferation with a mean GI50 value of 2.94 μM when screened against the NCI-60 panel of cancer cell lines and functions by blocking the G1/S phase of the cell cycle.{33362}  

     

    Brand:
    Cayman
    SKU:21273 -

    Out of stock

  • UF010 is a class I HDAC inhibitor with IC50 values of 0.06, 0.1, 0.5, and 1.5 µM for HDAC3, 2, 1, and 8, respectively.{33362} It is more than 6-fold selective for these class I HDACs over any additional HDACs.{33362} UF010 is reported to inhibit cancer cell proliferation with a mean GI50 value of 2.94 μM when screened against the NCI-60 panel of cancer cell lines and functions by blocking the G1/S phase of the cell cycle.{33362}  

     

    Brand:
    Cayman
    SKU:21273 -

    Out of stock

  • UK 1 is a metabolite from Streptomyces sp. 517-02 that demonstrates cytotoxic activity against various cancer cell lines, though it does not have antibacterial effects.{31697} It has been shown to inhibit topoisomerase II and also to inhibit hepatitis C viral replication.{31696,31698}  

     

    Brand:
    Cayman
    SKU:20139 -

    Available on backorder

  • UK 1 is a metabolite from Streptomyces sp. 517-02 that demonstrates cytotoxic activity against various cancer cell lines, though it does not have antibacterial effects.{31697} It has been shown to inhibit topoisomerase II and also to inhibit hepatitis C viral replication.{31696,31698}  

     

    Brand:
    Cayman
    SKU:20139 -

    Available on backorder

  • UK 371804 is an inhibitor of urokinase-type plasminogen activator (uPA; Ki = 10 nM).{45664} It is 4,000- and 2,700-fold selective for uPA over tissue plasminogen activator (tPA) and plasmin, respectively. UK 371804 inhibits exogenous uPA in human chronic wound fluid (IC50 = 0.89 μM). Topical administration of UK 371804 inhibits exogenous uPA activity in a porcine excisional wound model.  

     

    Brand:
    Cayman
    SKU:27225 - 10 mg

    Available on backorder

  • UK 371804 is an inhibitor of urokinase-type plasminogen activator (uPA; Ki = 10 nM).{45664} It is 4,000- and 2,700-fold selective for uPA over tissue plasminogen activator (tPA) and plasmin, respectively. UK 371804 inhibits exogenous uPA in human chronic wound fluid (IC50 = 0.89 μM). Topical administration of UK 371804 inhibits exogenous uPA activity in a porcine excisional wound model.  

     

    Brand:
    Cayman
    SKU:27225 - 25 mg

    Available on backorder

  • UK 371804 is an inhibitor of urokinase-type plasminogen activator (uPA; Ki = 10 nM).{45664} It is 4,000- and 2,700-fold selective for uPA over tissue plasminogen activator (tPA) and plasmin, respectively. UK 371804 inhibits exogenous uPA in human chronic wound fluid (IC50 = 0.89 μM). Topical administration of UK 371804 inhibits exogenous uPA activity in a porcine excisional wound model.  

     

    Brand:
    Cayman
    SKU:27225 - 5 mg

    Available on backorder

  • UK 383367 is a potent inhibitor of bone morphogenetic protein 1 (BMP1; IC50 = 44 nM).{31912,31911} It is more than 200-fold selective for BMP1 over a panel of matrix metalloproteinases. UK 383367 is effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.{31911}  

     

    Brand:
    Cayman
    SKU:-
  • UK 383367 is a potent inhibitor of bone morphogenetic protein 1 (BMP1; IC50 = 44 nM).{31912,31911} It is more than 200-fold selective for BMP1 over a panel of matrix metalloproteinases. UK 383367 is effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.{31911}  

     

    Brand:
    Cayman
    SKU:-
  • UK 383367 is a potent inhibitor of bone morphogenetic protein 1 (BMP1; IC50 = 44 nM).{31912,31911} It is more than 200-fold selective for BMP1 over a panel of matrix metalloproteinases. UK 383367 is effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.{31911}  

     

    Brand:
    Cayman
    SKU:-
  • UK 383367 is a potent inhibitor of bone morphogenetic protein 1 (BMP1; IC50 = 44 nM).{31912,31911} It is more than 200-fold selective for BMP1 over a panel of matrix metalloproteinases. UK 383367 is effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.{31911}  

     

    Brand:
    Cayman
    SKU:-
  • UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) that inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50 = 50 nM).{28011} It decreases glucose flux to the TCA cycle and increases production of M6 citrate via glutaminolytic flux through malic enzymes without affecting ATP-linked or uncoupled oxygen consumption in C2C12 myotubes when used at a concentration of 10 mM.{47146} UK 5099 decreases ATP-linked and uncoupled oxygen consumption in C2C12 myotubes when used in combination with BPTES (Item No. 19284) and/or etomoxir (Item No. 11969).  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) that inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50 = 50 nM).{28011} It decreases glucose flux to the TCA cycle and increases production of M6 citrate via glutaminolytic flux through malic enzymes without affecting ATP-linked or uncoupled oxygen consumption in C2C12 myotubes when used at a concentration of 10 mM.{47146} UK 5099 decreases ATP-linked and uncoupled oxygen consumption in C2C12 myotubes when used in combination with BPTES (Item No. 19284) and/or etomoxir (Item No. 11969).  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) that inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50 = 50 nM).{28011} It decreases glucose flux to the TCA cycle and increases production of M6 citrate via glutaminolytic flux through malic enzymes without affecting ATP-linked or uncoupled oxygen consumption in C2C12 myotubes when used at a concentration of 10 mM.{47146} UK 5099 decreases ATP-linked and uncoupled oxygen consumption in C2C12 myotubes when used in combination with BPTES (Item No. 19284) and/or etomoxir (Item No. 11969).  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) that inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50 = 50 nM).{28011} It decreases glucose flux to the TCA cycle and increases production of M6 citrate via glutaminolytic flux through malic enzymes without affecting ATP-linked or uncoupled oxygen consumption in C2C12 myotubes when used at a concentration of 10 mM.{47146} UK 5099 decreases ATP-linked and uncoupled oxygen consumption in C2C12 myotubes when used in combination with BPTES (Item No. 19284) and/or etomoxir (Item No. 11969).  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:23657 - 10 mg

    Available on backorder

  • Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:23657 - 25 mg

    Available on backorder

  • Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:23657 - 5 mg

    Available on backorder

  • Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SKOV3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:23657 - 50 mg

    Available on backorder

  • Ulipristal acetate-d6 is intended for use as an internal standard for the quantification of ulipristal acetate (Item No. 23657) by GC- or LC-MS. Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SK-OV-3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:26446 - 1 mg

    Available on backorder

  • Ulipristal acetate-d6 is intended for use as an internal standard for the quantification of ulipristal acetate (Item No. 23657) by GC- or LC-MS. Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC50s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC50 = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC50 = 15.4 nM).{40657} It is selective for human progesterone receptors over the human estrogen receptor (ER; EC50 = >10,000 nM). It inhibits growth of IGROV-1 and SK-OV-3 human ovarian cancer cells (IC50s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin (Item No. 13119) and paclitaxel (Item No. 10461) treatment has developed.{40658} Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.{40659} Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.{40660} Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.  

     

    Brand:
    Cayman
    SKU:26446 - 500 µg

    Available on backorder

  • Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC50 value of V600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC50s = 4.1 and 0.14 μM, respectively).{31542} Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC50 value of 180 nM.{31542}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC50 value of V600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC50s = 4.1 and 0.14 μM, respectively).{31542} Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC50 value of 180 nM.{31542}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC50 value of V600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC50s = 4.1 and 0.14 μM, respectively).{31542} Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC50 value of 180 nM.{31542}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC50 value of V600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC50s = 4.1 and 0.14 μM, respectively).{31542} Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC50 value of 180 nM.{31542}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26188 - 1 mg

    Available on backorder

  • UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26188 - 10 mg

    Available on backorder

  • UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26188 - 25 mg

    Available on backorder

  • UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.  

     

    Brand:
    Cayman
    SKU:26188 - 5 mg

    Available on backorder

  • UMB-32 is an inhibitor of the BET bromodomain BRD4 (Kd = 550 nM; IC50 = 637 nM) and the bromodomain-containing transcription factor TAF1 (Kd = 560 nM) and TAF1L (Kd = 1.3 µM).{27813}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UMB-32 is an inhibitor of the BET bromodomain BRD4 (Kd = 550 nM; IC50 = 637 nM) and the bromodomain-containing transcription factor TAF1 (Kd = 560 nM) and TAF1L (Kd = 1.3 µM).{27813}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UMB-32 is an inhibitor of the BET bromodomain BRD4 (Kd = 550 nM; IC50 = 637 nM) and the bromodomain-containing transcription factor TAF1 (Kd = 560 nM) and TAF1L (Kd = 1.3 µM).{27813}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UMB-32 is an inhibitor of the BET bromodomain BRD4 (Kd = 550 nM; IC50 = 637 nM) and the bromodomain-containing transcription factor TAF1 (Kd = 560 nM) and TAF1L (Kd = 1.3 µM).{27813}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Umbelliferone is a naturally occurring derivative and metabolite of coumarin that has diverse biological activities including antitumor, antioxidant, and antidepressant-like properties.{36671,36672,36673} It inhibits the growth of a variety of human cell lines, including human ACHN renal, A549 lung, HCT15 colon, and LNCaP prostate carcinoma as well as Dakiki myeloma and HL-60 lymphoma cells, when used at concentrations ranging from 250 to 300 µg/ml.{36671} It also reversibly inhibits the production of prostate-specific androgen in LNCaP prostate cancer cells. Umbelliferone increases the production of reactive oxygen species (ROS), depolarizes the mitochondrial membrane, and halts the cell cycle at the G0/G1 phase in KB human oral carcinoma cells.{36672} In a rat model of depression induced by chronic unpredictable mild stress, umbelliferone (15 and 30 mg/kg) decreases immobility time in the forced swim test and increases sucrose consumption in the sucrose preference test, indicating antidepressant-like activity.{36673} Umbelliferone has been used as a ratiometric pH indicator that displays an emission maxima of 460 nm when solutions with a pH of less than six or greater than eight are excited at 330 and 370 nm, respectively.{36674}  

     

    Brand:
    Cayman
    SKU:24665 - 100 mg

    Available on backorder

  • Umbelliferone is a naturally occurring derivative and metabolite of coumarin that has diverse biological activities including antitumor, antioxidant, and antidepressant-like properties.{36671,36672,36673} It inhibits the growth of a variety of human cell lines, including human ACHN renal, A549 lung, HCT15 colon, and LNCaP prostate carcinoma as well as Dakiki myeloma and HL-60 lymphoma cells, when used at concentrations ranging from 250 to 300 µg/ml.{36671} It also reversibly inhibits the production of prostate-specific androgen in LNCaP prostate cancer cells. Umbelliferone increases the production of reactive oxygen species (ROS), depolarizes the mitochondrial membrane, and halts the cell cycle at the G0/G1 phase in KB human oral carcinoma cells.{36672} In a rat model of depression induced by chronic unpredictable mild stress, umbelliferone (15 and 30 mg/kg) decreases immobility time in the forced swim test and increases sucrose consumption in the sucrose preference test, indicating antidepressant-like activity.{36673} Umbelliferone has been used as a ratiometric pH indicator that displays an emission maxima of 460 nm when solutions with a pH of less than six or greater than eight are excited at 330 and 370 nm, respectively.{36674}  

     

    Brand:
    Cayman
    SKU:24665 - 25 mg

    Available on backorder

  • Umbelliferone is a naturally occurring derivative and metabolite of coumarin that has diverse biological activities including antitumor, antioxidant, and antidepressant-like properties.{36671,36672,36673} It inhibits the growth of a variety of human cell lines, including human ACHN renal, A549 lung, HCT15 colon, and LNCaP prostate carcinoma as well as Dakiki myeloma and HL-60 lymphoma cells, when used at concentrations ranging from 250 to 300 µg/ml.{36671} It also reversibly inhibits the production of prostate-specific androgen in LNCaP prostate cancer cells. Umbelliferone increases the production of reactive oxygen species (ROS), depolarizes the mitochondrial membrane, and halts the cell cycle at the G0/G1 phase in KB human oral carcinoma cells.{36672} In a rat model of depression induced by chronic unpredictable mild stress, umbelliferone (15 and 30 mg/kg) decreases immobility time in the forced swim test and increases sucrose consumption in the sucrose preference test, indicating antidepressant-like activity.{36673} Umbelliferone has been used as a ratiometric pH indicator that displays an emission maxima of 460 nm when solutions with a pH of less than six or greater than eight are excited at 330 and 370 nm, respectively.{36674}  

     

    Brand:
    Cayman
    SKU:24665 - 50 mg

    Available on backorder

  • Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).  

     

    Brand:
    Cayman
    SKU:20700 -

    Available on backorder

  • Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).  

     

    Brand:
    Cayman
    SKU:20700 -

    Available on backorder

  • Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors).{39900,39902} It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 = 0.02 µg).{39900,39901} Formulations containing umeclidinium have been used in the treatment of chronic obstructive pulmonary disease (COPD).  

     

    Brand:
    Cayman
    SKU:20700 -

    Available on backorder

  • Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}  

     

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    Cayman
    SKU:-

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  • Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Umifenovir is a broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells. Because umifenovir targets a common critical step for viral replication, it is effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).{27500} Besides its antiviral action, umifenovir has been reported to produce an immunomodulatory response by inducing interferon production and stimulating the phagocytic function of macrophages.{27500}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Umirolimus is a semi-synthetic macrocyclic lactone and a derivative of rapamycin (Item No. 13346) that has immunosuppressive and anti-inflammatory effects.{36314} It halts the cell cycle at the G1 phase through an IL-2/mTOR-mediated pathway and inhibits proliferation of human smooth muscle cells. In a porcine overstretch model, coronary stents containing umirolimus for localized delivery to the vessel wall reduced stenosis by 50% and led to less thickening of the vessel wall than a bare metal stent. Rapamycin, and likely its derivatives, binds to the cytosolic FK-binding protein 12 (FKBP12) to inhibit the mammalian target of rapamycin (mTOR) pathway. Formulations containing umirolimus have been used in coronary stents for localized delivery to the vessel wall.  

     

    Brand:
    Cayman
    SKU:23585 - 1 mg

    Available on backorder

  • Umirolimus is a semi-synthetic macrocyclic lactone and a derivative of rapamycin (Item No. 13346) that has immunosuppressive and anti-inflammatory effects.{36314} It halts the cell cycle at the G1 phase through an IL-2/mTOR-mediated pathway and inhibits proliferation of human smooth muscle cells. In a porcine overstretch model, coronary stents containing umirolimus for localized delivery to the vessel wall reduced stenosis by 50% and led to less thickening of the vessel wall than a bare metal stent. Rapamycin, and likely its derivatives, binds to the cytosolic FK-binding protein 12 (FKBP12) to inhibit the mammalian target of rapamycin (mTOR) pathway. Formulations containing umirolimus have been used in coronary stents for localized delivery to the vessel wall.  

     

    Brand:
    Cayman
    SKU:23585 - 5 mg

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  • This EIA so called Easy Sampling EIA kit works with any sample collected on any kind of protease inhibitors, without extraction but a simple dilution. Ghrelin discovered in 1999, is fast becoming an endocrinology target of the millennium. Ghrelin, identified in rat stomach as an endogenous ligand for the GH secretagogue receptor, is mainly produced in stomach, but has been demonstrated in many otther organs. In addition to GH-releasing properties and its orexant action, Ghrelin could act as an hormone having effects on gastric motility (similarity with the peptide hormone motilin), acidic secretion, cardiovascular action, antiproliferative effects, pancreatic and glucose metabolism function, sleep… Ghrelin gene raises to mRNA prepro-ghrelin of 117 amino acids. This precursor is processed into Ghrelin, 28 amino acids (human). Before being secreted, this peptide is octanoylated at Ser 3 by GOAT (Ghrelin Octanoyl Acyl Transferase). This step is essential for biological activity making GOAT a perfect target for drugs in feeding behaviour. Interestingly, the potential therapeutic importance of this hormone is not restricted to regulation of food intake but also in cachexia (related to cancer treatment, anorexia nervosa or ischemia) gastric motility and may be involved in osteoporosis, somatopause, infertility and ovulation induction, neurological disorders (Alcoholism, Post Traumatic Stress disorders…) and cardiovascular diseases. [Bertin Catalog No. A05320.96 wells]  

     

    Brand:
    Cayman
    SKU:501200 - 96 wells

    Available on backorder

  • This EIA so called Easy Sampling EIA kit works with any sample collected on any kind of protease inhibitors, without extraction but a simple dilution. Ghrelin discovered in 1999, is fast becoming an endocrinology target of the millennium. Ghrelin, identified in rat stomach as an endogenous ligand for the GH secretagogue receptor, is mainly produced in stomach, but has been demonstrated in many other organs. In addition to GH-releasing properties and its orexant action, Ghrelin could act as an hormone having effects on gastric motility (similarity with the peptide hormone motilin), acidic secretion, cardiovascular action, antiproliferative effects, pancreatic and glucose metabolism function, sleep… Ghrelin gene raises to mRNA prepro-ghrelin of 117 amino acids. This precursor is processed into Ghrelin, 28 amino acids (human). Before being secreted, this peptide is octanoylated at Ser 3 by GOAT (Ghrelin Octanoyl Acyl Transferase). This step is essential for biological activity making GOAT a perfect target for drugs in feeding behaviour. Interestingly, the potential therapeutic importance of this hormone is not restricted to regulation of food intake but also in cachexia (related to cancer treatment, anorexia nervosa or ischemia) gastric motility and may be involved in osteoporosis, somatopause, infertility and ovulation induction, neurological disorders (Alcoholism, Post Traumatic Stress disorders…) and cardiovascular diseases. [Bertin Catalog No. A05319.96 wells]  

     

    Brand:
    Cayman
    SKU:501190 - 96 wells

    Available on backorder

  • Ghrelin, an endogenous ligand for the growth hormone secretagogue receptor, is synthesized principally in the stomach. It stimulates food intake and transduces signals to hypothalamic regulatory nucleid that controls energy homeostasis. The peptide consists of 28 amino acids, with a n-octanoylation of the serine-3 residue, which is necessary for biological activity. Ghrelin is present in the peripheral circulation in two forms: acylated and unacylated. This EIA kit specifically measures the unacylated form of ghrelin. Each kit contains ghrelin (unacylated) AChE-Fab’ conjugate, human unacylated ghrelin standard, human unacylated ghrelin quality control, Ellman’s reagent, EIA buffer, wash buffer, Tween 20, plates pre-coated with anti-ghrelin mouse monoclonal antibody, and complete instructions. [Bertin Catalog No. A05119]  

     

    Brand:
    Cayman
    SKU:10008952 - 96 wells

    Available on backorder

  • This EIA so called Easy Sampling EIA kit works with any sample collected on any kind of protease inhibitors, without extraction but a simple dilution. Ghrelin discovered in 1999, is fast becoming an endocrinology target of the millennium. Ghrelin, identified in rat stomach as an endogenous ligand for the GH secretagogue receptor, is mainly produced in stomach, but has been demonstrated in many other organs. In addition to GH-releasing properties and its orexant action, Ghrelin could act as an hormone having effects on gastric motility (similarity with the peptide hormone motilin), acidic secretion, cardiovascular action, antiproliferative effects, pancreatic and glucose metabolism function, sleep… Ghrelin gene raises to mRNA prepro-ghrelin of 117 amino acids. This precursor is processed into Ghrelin, 28 amino acids (human). Before being secreted, this peptide is octanoylated at Ser 3 by GOAT (Ghrelin Octanoyl Acyl Transferase). This step is essential for biological activity making GOAT a perfect target for drugs in feeding behaviour. Interestingly, the potential therapeutic importance of this hormone is not restricted to regulation of food intake but also in cachexia (related to cancer treatment, anorexia nervosa or ischemia) gastric motility and may be involved in osteoporosis, somatopause, infertility and ovulation induction, neurological disorders (Alcoholism, Post Traumatic Stress disorders…) and cardiovascular diseases. [Bertin Catalog No. A05318.96 wells]  

     

    Brand:
    Cayman
    SKU:501180 - 96 wells

    Available on backorder

  • Ghrelin, an endogenous ligand for the growth hormone secretagogue receptor, is synthesized principally in the stomach. It stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. The peptide consists of 28 amino acids, with an octanoylation of the serine-3 residue, which is necessary for biological activity. Ghrelin is present in the peripheral circulation in two forms: acylated and unacylated. This EIA kit specifically measures the unacylated form of ghrelin. Each kit contains ghrelin (unacylated) AChE-Fab’ conjugate, rat unacylated ghrelin standard, rat unacylated ghrelin quality control, Ellman’s reagent, EIA buffer, wash buffer, Tween 20, plates pre-coated with anti-ghrelin mouse monoclonal antibody, and complete instructions. [Bertin Catalog No. A05118]  

     

    Brand:
    Cayman
    SKU:10008953 - 96 wells

    Available on backorder

  • Ghrelin discovered in 1999, is fast becoming an endocrinology target of the millennium. Ghrelin, identified in rat stomach as an endogenous ligand for the GH secretagogue receptor, is mainly produced in stomach, but has been demonstrated in many otther organs. In addition to GH-releasing properties and its orexant action, Ghrelin could act as an hormone having effects on gastric motility (similarity with the peptide hormone motilin), acidic secretion, cardiovascular action, antiproliferative effects, pancreatic and glucose metabolism function, sleep… Ghrelin gene raises to mRNA prepro-ghrelin of 117 amino acids. This precursor is processed into Ghrelin, 28 amino acids (human). Before being secreted, this peptide is octanoylated at Ser 3 by GOAT (Ghrelin Octanoyl Acyl Transferase). This step is essential for biological activity making GOAT a perfect target for drugs in feeding behaviour. Interestingly, the potential therapeutic importance of this hormone is not restricted to regulation of food intake but also in cachexia (related to cancer treatment, anorexia nervosa or ischemia) gastric motility and may be involved in osteoporosis, somatopause, infertility and ovulation induction, neurological disorders (Alcoholism, Post Traumatic Stress disorders…) and cardiovascular diseases. [Bertin Catalog No. A05402.96 wells]  

     

    Brand:
    Cayman
    SKU:501230 - 96 wells

    Available on backorder

  • UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • UNBS5162 is a naphthalimide that antagonizes the expression of CXCL chemokines. In vitro exposure of PC-3 prostate cancer cells to 1 µM UNBS5162 for five successive days was shown to decrease the expression of proangiogenic CXCL chemokines.{32670} UNBS5162 also demonstrates antiangiogenic properties in vivo in an orthotopic PC-3 model.{32670}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}  

     

    Brand:
    Cayman
    SKU:-
  • SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM).{26523} It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 µM).{26523}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}  

     

    Brand:
    Cayman
    SKU:11084 - 1 mg

    Available on backorder

  • UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}  

     

    Brand:
    Cayman
    SKU:11084 - 10 mg

    Available on backorder

  • UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}  

     

    Brand:
    Cayman
    SKU:11084 - 25 mg

    Available on backorder

  • UNC0631 is a potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).{19978} It potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 cell line.{19978}  

     

    Brand:
    Cayman
    SKU:11084 - 5 mg

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:10734 - 1 mg

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:10734 - 10 mg

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:10734 - 5 mg

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:10734 - 50 mg

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}  

     

    Brand:
    Cayman
    SKU:11085 - 1 mg

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  • G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}  

     

    Brand:
    Cayman
    SKU:11085 - 10 mg

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  • G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}  

     

    Brand:
    Cayman
    SKU:11085 - 5 mg

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  • G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}  

     

    Brand:
    Cayman
    SKU:11085 - 50 mg

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  • UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:20566 -

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  • UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:20566 -

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  • UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:20566 -

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  • UNC1079 is an analog of UNC1215 (Item No. 13968), the selective L3MBTL3 domain inhibitor. UNC1079 is a 1,000-fold weaker than UNC1215 as a L3MBTL3 domain inhibitor.{22123} This compound is intended for use as a negative control in cellular studies.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
    SKU:20566 -

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  • Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
    SKU:-
  • Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors.{22123} UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides.{22123} This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined.{22123} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-
  • The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.  

     

    Brand:
    Cayman
    SKU:-
  • The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.  

     

    Brand:
    Cayman
    SKU:-
  • The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.  

     

    Brand:
    Cayman
    SKU:-
  • The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{25004} UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.{25004} For more information on UNC1999 please visit the Structural Genomics Consortium (SGC). The negative control, UNC2400, for UNC1999 is also available exclusively through the SGC. You can submit a request to receive the negative control here.  

     

    Brand:
    Cayman
    SKU:-
  • UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).{26933} It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.{26933} UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.{26933} Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.{26933}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}  

     

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    Cayman
    SKU:-

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  • Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}  

     

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    Cayman
    SKU:-

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  • UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3; IC50 = 230 nM).{30116}  

     

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    Cayman
    SKU:-

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