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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}
Brand:CaymanSKU:13724 - 200 µgAvailable on backorder
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:CaymanSKU:13724- 200 µgAvailable on backorder
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:CaymanSKU:13724- 200 µgUbiquitin 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}
Brand:CaymanSKU:13724 - 50 µgAvailable on backorder
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:CaymanSKU:13724- 50 µgAvailable on backorder
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:CaymanSKU:13724- 50 µgUBP 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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:24309 - 1 mgAvailable on backorder
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}
Brand:CaymanSKU:24309 - 5 mgAvailable on backorder
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.
Brand:CaymanSKU:21806 -Out of stock
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.
Brand:CaymanSKU:21806 -Out of stock
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.
Brand:CaymanSKU:21806 -Out of stock
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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:10045 - 10 mgAvailable on backorder
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}
Brand:CaymanSKU:10045 - 25 mgAvailable on backorder
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}
Brand:CaymanSKU:10045 - 5 mgAvailable on backorder
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}
Brand:CaymanSKU:10045 - 50 mgAvailable on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:20221 -Available on backorder
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}
Brand:CaymanSKU:20221 -Available on backorder
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}
Brand:CaymanSKU:21460 -Out of stock
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}
Brand:CaymanSKU:21460 -Out of stock
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}
Brand:CaymanSKU:21460 -Out of stock
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}
Brand:CaymanSKU:30373 - 10 mgAvailable on backorder
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}
Brand:CaymanSKU:30373 - 25 mgAvailable on backorder
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}
Brand:CaymanSKU:30373 - 5 mgAvailable on backorder
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}
Brand:CaymanSKU:30373 - 50 mgAvailable on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:-Available on backorder
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}
Brand:CaymanSKU:20353 -Available on backorder
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}
Brand:CaymanSKU:20353 -Available on backorder
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}
Brand:CaymanSKU:20353 -Available on backorder
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}
Brand:CaymanSKU:-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}
Brand:CaymanSKU:-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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:27225 - 10 mgAvailable 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:CaymanSKU:27225 - 25 mgAvailable 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:CaymanSKU:27225 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:23657 - 10 mgAvailable 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:CaymanSKU:23657 - 25 mgAvailable 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:CaymanSKU:23657 - 5 mgAvailable 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:CaymanSKU:23657 - 50 mgAvailable 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:CaymanSKU:26446 - 1 mgAvailable 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:CaymanSKU:26446 - 500 µgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:26188 - 1 mgAvailable 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:CaymanSKU:26188 - 10 mgAvailable 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:CaymanSKU:26188 - 25 mgAvailable 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:CaymanSKU:26188 - 5 mgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-Out of stock