Cayman

Showing 26551–26700 of 45550 results

  • Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins.{28729,28730} It is much less effective or without effect against a panel of 229 other kinases.{28729} Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.{28729,28730} It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme.{28728} Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.{28728,28731}  

     

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    Cayman
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  • Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}  

     

    Brand:
    Cayman
    SKU:25139 - 1 mg

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  • Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}  

     

    Brand:
    Cayman
    SKU:25139 - 10 mg

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  • Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}  

     

    Brand:
    Cayman
    SKU:25139 - 5 mg

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  • Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}  

     

    Brand:
    Cayman
    SKU:21091 -

    Out of stock

  • Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}  

     

    Brand:
    Cayman
    SKU:21091 -

    Out of stock

  • Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}  

     

    Brand:
    Cayman
    SKU:21091 -

    Out of stock

  • Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}  

     

    Brand:
    Cayman
    SKU:21091 -

    Out of stock

  • Kumbicin C is a bis-indolyl benzenoid fungal metabolite produced by A. kumbius FRR6049.{39715} It inhibits the growth of NS-1 mouse myeloma cells (IC50 = 0.74 μg/ml). Kumbicin C also inhibits the growth of the Gram-positive bacteria B. subtilis (MIC = 1.6 μg/ml).  

     

    Brand:
    Cayman
    SKU:25015 - 1 mg

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  • Kumbicin C is a bis-indolyl benzenoid fungal metabolite produced by A. kumbius FRR6049.{39715} It inhibits the growth of NS-1 mouse myeloma cells (IC50 = 0.74 μg/ml). Kumbicin C also inhibits the growth of the Gram-positive bacteria B. subtilis (MIC = 1.6 μg/ml).  

     

    Brand:
    Cayman
    SKU:25015 - 250 µg

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  • KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}  

     

    Brand:
    Cayman
    SKU:30297 - 1 mg

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  • KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}  

     

    Brand:
    Cayman
    SKU:30297 - 10 mg

    Available on backorder

  • KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}  

     

    Brand:
    Cayman
    SKU:30297 - 5 mg

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  • Ion channels are integral membrane proteins that help establish and control the small voltage gradient across the plasma membrane of living cells by allowing the flow of ions down their electrochemical gradient.{17533} They are present in the membranes that surround all biological cells and their main function is to regulate the flow of ions across this membrane. Whereas some ion channels permit the passage of ions based on charge, others conduct based on a ionic species, such as sodium or potassium. Furthermore, in some ion channels, the passage is governed by a gate which is controlled by chemical or electrical signals, temperature, or mechanical forces. There are a few main classifications of gated ion channels. There are voltage-gated ion channels, ligand-gated, other gating systems, and finally those that are classified differently, having more exotic characteristics. The first are voltage-gated ion channels which open and close in response to membrane potential. These are then seperated into sodium, calcium, potassium, proton, transient receptor, and cyclic nucleotide-gated channels, each of which is responsible for a unique role. Ligand-gated ion channels are also known as ionotropic receptors and they open in response to specific ligand molecules binding to the extracellular domain of the receptor protein. The other gated classifications include activation and inactivation by second messengers, inward-rectifier potassium channels, calcium-activated potassium channels, two-pore-domain potassium channels, light-gated channels, mechano-sensitive ion channels, and cyclic nucleotide-gated channels. Finally, the other classifications are based on less normal characteristics such as two-pore channels and transient receptor potential channels.{17535} Potassium voltage-gated channel, Shaw-related subfamily, member 1, also known as KCNC1 or Kv3.1, is a human gene. The Shaker gene family of Drosophila encodes components of voltage-gated potassium channels and is comprised of four subfamilies. Based in sequence similarity, this gene is similar to one of these subfamilies, namely the Shaw subfamily.{17687} The protein encoded by this gene belongs to the delayed rectifier class of channel proteins and is an integral membrane protein that mediates the voltage-dependent potassium ion permeability of excitable membranes. Kv3.1b has been extensively tested in the auditory regions of mammals, and the decline of Kv3.1b expression appears to correlate with the functional decline in the medial olivocochlear efferent system.{17688} Other research shows potential for Kv3.1b channels to be oxygen sensors.{17689}  

     

    Brand:
    Cayman
    SKU:13717 - 100 µg

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  • Antigen: fusion protein amino acids 437-585 of rat Kv3.1b • Host: mouse, clone S16B-8 • Isotype: IgG1 • Cross Reactivity: (+) human, mouse, and rat Kv3.1b • Application(s): IHC and WB • Kv3.1b has been extensively tested in the auditory regions of mammals, and the decline of Kv3.1b expression appears to correlate with the functional decline in the medial olivocochlear efferent system. Other research shows potential for Kv3.1b channels to be oxygen sensors.  

     

    Brand:
    Cayman
    SKU:13717- 100 µg

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  • Antigen: fusion protein amino acids 437-585 of rat Kv3.1b • Host: mouse, clone S16B-8 • Isotype: IgG1 • Cross Reactivity: (+) human, mouse, and rat Kv3.1b • Application(s): IHC and WB • Kv3.1b has been extensively tested in the auditory regions of mammals, and the decline of Kv3.1b expression appears to correlate with the functional decline in the medial olivocochlear efferent system. Other research shows potential for Kv3.1b channels to be oxygen sensors.  

     

    Brand:
    Cayman
    SKU:13717- 100 µg
  • KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.  

     

    Brand:
    Cayman
    SKU:22207 -

    Out of stock

  • KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.  

     

    Brand:
    Cayman
    SKU:22207 -

    Out of stock

  • KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.  

     

    Brand:
    Cayman
    SKU:22207 -

    Out of stock

  • KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.  

     

    Brand:
    Cayman
    SKU:22207 -

    Out of stock

  • KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22418 -

    Out of stock

  • KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22418 -

    Out of stock

  • KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22418 -

    Out of stock

  • KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22418 -

    Out of stock

  • KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}  

     

    Brand:
    Cayman
    SKU:11940 - 1 mg

    Available on backorder

  • KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}  

     

    Brand:
    Cayman
    SKU:11940 - 10 mg

    Available on backorder

  • KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}  

     

    Brand:
    Cayman
    SKU:11940 - 25 mg

    Available on backorder

  • KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}  

     

    Brand:
    Cayman
    SKU:11940 - 5 mg

    Available on backorder

  • KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}  

     

    Brand:
    Cayman
    SKU:22198 -

    Out of stock

  • KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}  

     

    Brand:
    Cayman
    SKU:22198 -

    Out of stock

  • KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}  

     

    Brand:
    Cayman
    SKU:22198 -

    Out of stock

  • KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}  

     

    Brand:
    Cayman
    SKU:22198 -

    Out of stock

  • KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.  

     

    Brand:
    Cayman
    SKU:21429 -

    Out of stock

  • KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.  

     

    Brand:
    Cayman
    SKU:21429 -

    Out of stock

  • KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.  

     

    Brand:
    Cayman
    SKU:21429 -

    Out of stock

  • KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.  

     

    Brand:
    Cayman
    SKU:21429 -

    Out of stock

  • KY 02111 promotes the differentiation of human pluripotent stem cells to cardiomyocytes by inhibiting Wnt signaling.{24540} Treatment with 10 μM of KY 02111 has been shown to increase the ratio of beating cardiac colonies by 70–94% in cell aggregates of the embryonic stem cell lines KhES-1 and KhES-3 as well as the induced pluripotent stem cell lines 253G1, IMR90-1, IMR90-4, and RCHIPC0003.{24540}  

     

    Brand:
    Cayman
    SKU:-
  • KY 02111 promotes the differentiation of human pluripotent stem cells to cardiomyocytes by inhibiting Wnt signaling.{24540} Treatment with 10 μM of KY 02111 has been shown to increase the ratio of beating cardiac colonies by 70–94% in cell aggregates of the embryonic stem cell lines KhES-1 and KhES-3 as well as the induced pluripotent stem cell lines 253G1, IMR90-1, IMR90-4, and RCHIPC0003.{24540}  

     

    Brand:
    Cayman
    SKU:-
  • KY 02111 promotes the differentiation of human pluripotent stem cells to cardiomyocytes by inhibiting Wnt signaling.{24540} Treatment with 10 μM of KY 02111 has been shown to increase the ratio of beating cardiac colonies by 70–94% in cell aggregates of the embryonic stem cell lines KhES-1 and KhES-3 as well as the induced pluripotent stem cell lines 253G1, IMR90-1, IMR90-4, and RCHIPC0003.{24540}  

     

    Brand:
    Cayman
    SKU:-
  • KY 02111 promotes the differentiation of human pluripotent stem cells to cardiomyocytes by inhibiting Wnt signaling.{24540} Treatment with 10 μM of KY 02111 has been shown to increase the ratio of beating cardiac colonies by 70–94% in cell aggregates of the embryonic stem cell lines KhES-1 and KhES-3 as well as the induced pluripotent stem cell lines 253G1, IMR90-1, IMR90-4, and RCHIPC0003.{24540}  

     

    Brand:
    Cayman
    SKU:-
  • KY 05009 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; Ki = 100 nM).{47794} It inhibits TGF-β1-induced Wnt, NF-κB, ERK, and JNK signaling and prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in A549 lung cancer cells without inducing cytotoxicity when used at a concentration of 10 μM. KY 05009 inhibits TNF-β1-induced A549 cell migration. It also induces apoptosis in RPMI-8226 multiple myeloma cells in a concentration-dependent manner.{47795}  

     

    Brand:
    Cayman
    SKU:29552 - 1 mg

    Available on backorder

  • KY 05009 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; Ki = 100 nM).{47794} It inhibits TGF-β1-induced Wnt, NF-κB, ERK, and JNK signaling and prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in A549 lung cancer cells without inducing cytotoxicity when used at a concentration of 10 μM. KY 05009 inhibits TNF-β1-induced A549 cell migration. It also induces apoptosis in RPMI-8226 multiple myeloma cells in a concentration-dependent manner.{47795}  

     

    Brand:
    Cayman
    SKU:29552 - 10 mg

    Available on backorder

  • KY 05009 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; Ki = 100 nM).{47794} It inhibits TGF-β1-induced Wnt, NF-κB, ERK, and JNK signaling and prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in A549 lung cancer cells without inducing cytotoxicity when used at a concentration of 10 μM. KY 05009 inhibits TNF-β1-induced A549 cell migration. It also induces apoptosis in RPMI-8226 multiple myeloma cells in a concentration-dependent manner.{47795}  

     

    Brand:
    Cayman
    SKU:29552 - 25 mg

    Available on backorder

  • KY 05009 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; Ki = 100 nM).{47794} It inhibits TGF-β1-induced Wnt, NF-κB, ERK, and JNK signaling and prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in A549 lung cancer cells without inducing cytotoxicity when used at a concentration of 10 μM. KY 05009 inhibits TNF-β1-induced A549 cell migration. It also induces apoptosis in RPMI-8226 multiple myeloma cells in a concentration-dependent manner.{47795}  

     

    Brand:
    Cayman
    SKU:29552 - 5 mg

    Available on backorder

  • KYA1797K is an inhibitor of Wnt/β-catenin signaling.{46795} It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.  

     

    Brand:
    Cayman
    SKU:29221 - 10 mg

    Available on backorder

  • KYA1797K is an inhibitor of Wnt/β-catenin signaling.{46795} It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.  

     

    Brand:
    Cayman
    SKU:29221 - 25 mg

    Available on backorder

  • KYA1797K is an inhibitor of Wnt/β-catenin signaling.{46795} It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.  

     

    Brand:
    Cayman
    SKU:29221 - 5 mg

    Available on backorder

  • KYA1797K is an inhibitor of Wnt/β-catenin signaling.{46795} It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.  

     

    Brand:
    Cayman
    SKU:29221 - 50 mg

    Available on backorder

  • Kynurenic acid is a natural metabolite of tryptophan via the kynurenine pathway. It has pronounced effects on neuronal signaling and, thus, impacts diverse neurological systems.{27403,27404} Kynurenic acid broadly antagonizes ionotopic glutamate receptors at high micromolar to millimolar concentrations and is used to pharmacologically block the activation of these receptors in vivo or in vitro.{27407} In addition, it reportedly has more potent effects at glutamate receptor subunit ζ-1 (Ki = 5.4 µM), GPR35 (EC50 = 39 µM), aryl hydrocarbon receptor (EC50 = 300 nM), and neuronal acetylcholine receptor α-7 (IC50 = 7 µM).{27405,14771,27406,27404}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Kynurenic acid is a natural metabolite of tryptophan via the kynurenine pathway. It has pronounced effects on neuronal signaling and, thus, impacts diverse neurological systems.{27403,27404} Kynurenic acid broadly antagonizes ionotopic glutamate receptors at high micromolar to millimolar concentrations and is used to pharmacologically block the activation of these receptors in vivo or in vitro.{27407} In addition, it reportedly has more potent effects at glutamate receptor subunit ζ-1 (Ki = 5.4 µM), GPR35 (EC50 = 39 µM), aryl hydrocarbon receptor (EC50 = 300 nM), and neuronal acetylcholine receptor α-7 (IC50 = 7 µM).{27405,14771,27406,27404}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Kynurenic acid is a natural metabolite of tryptophan via the kynurenine pathway. It has pronounced effects on neuronal signaling and, thus, impacts diverse neurological systems.{27403,27404} Kynurenic acid broadly antagonizes ionotopic glutamate receptors at high micromolar to millimolar concentrations and is used to pharmacologically block the activation of these receptors in vivo or in vitro.{27407} In addition, it reportedly has more potent effects at glutamate receptor subunit ζ-1 (Ki = 5.4 µM), GPR35 (EC50 = 39 µM), aryl hydrocarbon receptor (EC50 = 300 nM), and neuronal acetylcholine receptor α-7 (IC50 = 7 µM).{27405,14771,27406,27404}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Kynurenine is a product of constitutive tryptophan catabolism via tryptophan-2,3-dioxygenase in the liver and human gliomas that is associated with the suppression of antitumor immune responses. At 100 μM, kynurenine inhibits allogeneic T-cell proliferation and increases malignant U87 glioma cell invasion into a collagen matrix.{20319} Kynurenine activates the aryl hydrocarbon receptor (AhR) target gene CYP1A1 with an EC50 value of 12.3 μM and binds to AhR with an apparent Kd value of ~4 μM.{20319} Kynurenine is ultimately metabolized to quinolinic acid, a potent neurotoxin that acts as an NMDA agonist and has been described to be involved in neurodegenerative processes in the brain.{20572}  

     

    Brand:
    Cayman
    SKU:11305 - 100 mg

    Available on backorder

  • Kynurenine is a product of constitutive tryptophan catabolism via tryptophan-2,3-dioxygenase in the liver and human gliomas that is associated with the suppression of antitumor immune responses. At 100 μM, kynurenine inhibits allogeneic T-cell proliferation and increases malignant U87 glioma cell invasion into a collagen matrix.{20319} Kynurenine activates the aryl hydrocarbon receptor (AhR) target gene CYP1A1 with an EC50 value of 12.3 μM and binds to AhR with an apparent Kd value of ~4 μM.{20319} Kynurenine is ultimately metabolized to quinolinic acid, a potent neurotoxin that acts as an NMDA agonist and has been described to be involved in neurodegenerative processes in the brain.{20572}  

     

    Brand:
    Cayman
    SKU:11305 - 250 mg

    Available on backorder

  • Kynurenine is a product of constitutive tryptophan catabolism via tryptophan-2,3-dioxygenase in the liver and human gliomas that is associated with the suppression of antitumor immune responses. At 100 μM, kynurenine inhibits allogeneic T-cell proliferation and increases malignant U87 glioma cell invasion into a collagen matrix.{20319} Kynurenine activates the aryl hydrocarbon receptor (AhR) target gene CYP1A1 with an EC50 value of 12.3 μM and binds to AhR with an apparent Kd value of ~4 μM.{20319} Kynurenine is ultimately metabolized to quinolinic acid, a potent neurotoxin that acts as an NMDA agonist and has been described to be involved in neurodegenerative processes in the brain.{20572}  

     

    Brand:
    Cayman
    SKU:11305 - 50 mg

    Available on backorder

  • Kynurenine is a product of constitutive tryptophan catabolism via tryptophan-2,3-dioxygenase in the liver and human gliomas that is associated with the suppression of antitumor immune responses. At 100 μM, kynurenine inhibits allogeneic T-cell proliferation and increases malignant U87 glioma cell invasion into a collagen matrix.{20319} Kynurenine activates the aryl hydrocarbon receptor (AhR) target gene CYP1A1 with an EC50 value of 12.3 μM and binds to AhR with an apparent Kd value of ~4 μM.{20319} Kynurenine is ultimately metabolized to quinolinic acid, a potent neurotoxin that acts as an NMDA agonist and has been described to be involved in neurodegenerative processes in the brain.{20572}  

     

    Brand:
    Cayman
    SKU:11305 - 500 mg

    Available on backorder

  • L-(–)-Norepinephrine is a natural neurotransmitter and hormone that is biosynthesized from dopamine by dopamine β-hydroxylase.{29553,29557} It is an agonist of adrenergic receptors (Ki values are 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively).{29557} Through these receptors, L-(–)-norepinephrine regulates diverse processes, including those in neurological, immunological, and vascular systems.{29557,29554,29555,29556}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • L-(–)-Norepinephrine is a natural neurotransmitter and hormone that is biosynthesized from dopamine by dopamine β-hydroxylase.{29553,29557} It is an agonist of adrenergic receptors (Ki values are 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively).{29557} Through these receptors, L-(–)-norepinephrine regulates diverse processes, including those in neurological, immunological, and vascular systems.{29557,29554,29555,29556}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • L-(–)-Norepinephrine is a natural neurotransmitter and hormone that is biosynthesized from dopamine by dopamine β-hydroxylase.{29553,29557} It is an agonist of adrenergic receptors (Ki values are 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively).{29557} Through these receptors, L-(–)-norepinephrine regulates diverse processes, including those in neurological, immunological, and vascular systems.{29557,29554,29555,29556}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • L-(–)-Norepinephrine is a natural neurotransmitter and hormone that is biosynthesized from dopamine by dopamine β-hydroxylase.{29553,29557} It is an agonist of adrenergic receptors (Ki values are 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively).{29557} Through these receptors, L-(–)-norepinephrine regulates diverse processes, including those in neurological, immunological, and vascular systems.{29557,29554,29555,29556}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • L-(–)-Sorbose is a monosaccharide and an intermediate in the biosynthesis of L-ascorbic acid (Item No. 14656) in bacteria.{46172,46173} It is formed via dehydrogenation of D-sorbitol by D-sorbitol dehydrogenase (SLDH).{46173} L-(–)-Sorbose has commonly been used as a starting material in the commercial biosynthesis of L-ascorbic acid.  

     

    Brand:
    Cayman
    SKU:26812 - 100 g

    Available on backorder

  • L-(–)-Sorbose is a monosaccharide and an intermediate in the biosynthesis of L-ascorbic acid (Item No. 14656) in bacteria.{46172,46173} It is formed via dehydrogenation of D-sorbitol by D-sorbitol dehydrogenase (SLDH).{46173} L-(–)-Sorbose has commonly been used as a starting material in the commercial biosynthesis of L-ascorbic acid.  

     

    Brand:
    Cayman
    SKU:26812 - 250 g

    Available on backorder

  • L-(–)-Sorbose is a monosaccharide and an intermediate in the biosynthesis of L-ascorbic acid (Item No. 14656) in bacteria.{46172,46173} It is formed via dehydrogenation of D-sorbitol by D-sorbitol dehydrogenase (SLDH).{46173} L-(–)-Sorbose has commonly been used as a starting material in the commercial biosynthesis of L-ascorbic acid.  

     

    Brand:
    Cayman
    SKU:26812 - 50 g

    Available on backorder

  • L-(+)-Cystathionine is a dipeptide formed by serine and homocysteine. Transsulfuration of methionine yields homocysteine, which combines with serine to form this precursor of cysteine.{17812,26041} L-(+)-Cystathionine is largely expressed in the mammalian brain and deficiency can indicate the presence of metabolic disorders such as cystathioninuria.{26040}  

     

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    Cayman
    SKU:-
  • L-(+)-Cystathionine is a dipeptide formed by serine and homocysteine. Transsulfuration of methionine yields homocysteine, which combines with serine to form this precursor of cysteine.{17812,26041} L-(+)-Cystathionine is largely expressed in the mammalian brain and deficiency can indicate the presence of metabolic disorders such as cystathioninuria.{26040}  

     

    Brand:
    Cayman
    SKU:-
  • L-(+)-Cystathionine is a dipeptide formed by serine and homocysteine. Transsulfuration of methionine yields homocysteine, which combines with serine to form this precursor of cysteine.{17812,26041} L-(+)-Cystathionine is largely expressed in the mammalian brain and deficiency can indicate the presence of metabolic disorders such as cystathioninuria.{26040}  

     

    Brand:
    Cayman
    SKU:-
  • L-(+)-Cystathionine is a dipeptide formed by serine and homocysteine. Transsulfuration of methionine yields homocysteine, which combines with serine to form this precursor of cysteine.{17812,26041} L-(+)-Cystathionine is largely expressed in the mammalian brain and deficiency can indicate the presence of metabolic disorders such as cystathioninuria.{26040}  

     

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    Cayman
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  • L-(+)-Ergothioneine is a naturally-occurring amino acid derived from histidine via hercynine.{23678} Ergothioneine is a stable antioxidant that scavenges and detoxifies free radicals and oxidants, increases intracellular thiol levels, controls nuclear factor-κB activation, and inhibits inflammatory gene expression.{23667,23665} In addition, it inhibits the peroxynitrite-dependent nitration of nitrotyrosine, blocks oxidative DNA damage and cell death, and prevents the formation of xanthine and hypoxanthine.{23667,23664,23668} Ergothioneine is transported by the organic cation/carnitine transporter 1, which has been linked with autoimmune diseases, including rheumatoid arthritis and Crohn’s disease.{23666}  

     

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    Cayman
    SKU:-
  • L-(+)-Ergothioneine is a naturally-occurring amino acid derived from histidine via hercynine.{23678} Ergothioneine is a stable antioxidant that scavenges and detoxifies free radicals and oxidants, increases intracellular thiol levels, controls nuclear factor-κB activation, and inhibits inflammatory gene expression.{23667,23665} In addition, it inhibits the peroxynitrite-dependent nitration of nitrotyrosine, blocks oxidative DNA damage and cell death, and prevents the formation of xanthine and hypoxanthine.{23667,23664,23668} Ergothioneine is transported by the organic cation/carnitine transporter 1, which has been linked with autoimmune diseases, including rheumatoid arthritis and Crohn’s disease.{23666}  

     

    Brand:
    Cayman
    SKU:-
  • L-(+)-Ergothioneine is a naturally-occurring amino acid derived from histidine via hercynine.{23678} Ergothioneine is a stable antioxidant that scavenges and detoxifies free radicals and oxidants, increases intracellular thiol levels, controls nuclear factor-κB activation, and inhibits inflammatory gene expression.{23667,23665} In addition, it inhibits the peroxynitrite-dependent nitration of nitrotyrosine, blocks oxidative DNA damage and cell death, and prevents the formation of xanthine and hypoxanthine.{23667,23664,23668} Ergothioneine is transported by the organic cation/carnitine transporter 1, which has been linked with autoimmune diseases, including rheumatoid arthritis and Crohn’s disease.{23666}  

     

    Brand:
    Cayman
    SKU:-
  • L-(+)-Ergothioneine is a naturally-occurring amino acid derived from histidine via hercynine.{23678} Ergothioneine is a stable antioxidant that scavenges and detoxifies free radicals and oxidants, increases intracellular thiol levels, controls nuclear factor-κB activation, and inhibits inflammatory gene expression.{23667,23665} In addition, it inhibits the peroxynitrite-dependent nitration of nitrotyrosine, blocks oxidative DNA damage and cell death, and prevents the formation of xanthine and hypoxanthine.{23667,23664,23668} Ergothioneine is transported by the organic cation/carnitine transporter 1, which has been linked with autoimmune diseases, including rheumatoid arthritis and Crohn’s disease.{23666}  

     

    Brand:
    Cayman
    SKU:-
  • L-(+)-Erythrose is an aldotetrose carbohydrate that has been used in glycation studies and to characterize erythrose reductase activity.{32093,32092}  

     

    Brand:
    Cayman
    SKU:20381 -

    Available on backorder

  • L-(+)-Erythrose is an aldotetrose carbohydrate that has been used in glycation studies and to characterize erythrose reductase activity.{32093,32092}  

     

    Brand:
    Cayman
    SKU:20381 -

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  • L-(+)-Erythrose is an aldotetrose carbohydrate that has been used in glycation studies and to characterize erythrose reductase activity.{32093,32092}  

     

    Brand:
    Cayman
    SKU:20381 -

    Available on backorder

  • L-(+)-Erythrose is an aldotetrose carbohydrate that has been used in glycation studies and to characterize erythrose reductase activity.{32093,32092}  

     

    Brand:
    Cayman
    SKU:20381 -

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  • L-(−)-Fucose is a deoxyhexose monosaccharide found on N- and O-linked glycans and glycolipids of a wide variety of organisms.{26957} It can exist as a terminal modification of glycan structures or serve as a point of attachment for adding other sugars.{26958} In humans, L-(−)-fucose plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.{26957}  

     

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    Cayman
    SKU:-

    Out of stock

  • L-(−)-Fucose is a deoxyhexose monosaccharide found on N- and O-linked glycans and glycolipids of a wide variety of organisms.{26957} It can exist as a terminal modification of glycan structures or serve as a point of attachment for adding other sugars.{26958} In humans, L-(−)-fucose plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.{26957}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • L-(−)-Fucose is a deoxyhexose monosaccharide found on N- and O-linked glycans and glycolipids of a wide variety of organisms.{26957} It can exist as a terminal modification of glycan structures or serve as a point of attachment for adding other sugars.{26958} In humans, L-(−)-fucose plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.{26957}  

     

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    Cayman
    SKU:-

    Out of stock

  • L-(−)-Glucose is an enantiomer of the more common D-glucose. L-Glucose is not bioavailable to cells as an energy source because it cannot be phosphorylated by hexokinase. However, certain L-glucose-utilizing bacteria that contain NAD+-dependent L-glucose dehydrogenases capable of oxidizing L-glucose have been identified.{32647}  

     

    Brand:
    Cayman
    SKU:20829 -

    Out of stock

  • L-(−)-Glucose is an enantiomer of the more common D-glucose. L-Glucose is not bioavailable to cells as an energy source because it cannot be phosphorylated by hexokinase. However, certain L-glucose-utilizing bacteria that contain NAD+-dependent L-glucose dehydrogenases capable of oxidizing L-glucose have been identified.{32647}  

     

    Brand:
    Cayman
    SKU:20829 -

    Out of stock

  • L-(−)-Glucose is an enantiomer of the more common D-glucose. L-Glucose is not bioavailable to cells as an energy source because it cannot be phosphorylated by hexokinase. However, certain L-glucose-utilizing bacteria that contain NAD+-dependent L-glucose dehydrogenases capable of oxidizing L-glucose have been identified.{32647}  

     

    Brand:
    Cayman
    SKU:20829 -

    Out of stock

  • L-(−)-α-Methyldopa is a dopamine (DOPA) decarboxylase inhibitor (ED50 = 21.8 mg/kg) and has antihypertensive activity in vitro and in vivo.{36001,36002,36000} L-(−)-α-Methyldopa enters the CNS and is metabolized to form α-methylnorepinephrine which acts as an agonist at α2-adrenergic receptors.{36001,36000} Formulations containing L-(−)-α-methyldopa are used to lower blood pressure.{36002} L-(−)-α-Methyldopa also improves trophoblast and endothelial cellular interactions in vitro.{36001}  

     

    Brand:
    Cayman
    SKU:21814 -

    Out of stock

  • L-(−)-α-Methyldopa is a dopamine (DOPA) decarboxylase inhibitor (ED50 = 21.8 mg/kg) and has antihypertensive activity in vitro and in vivo.{36001,36002,36000} L-(−)-α-Methyldopa enters the CNS and is metabolized to form α-methylnorepinephrine which acts as an agonist at α2-adrenergic receptors.{36001,36000} Formulations containing L-(−)-α-methyldopa are used to lower blood pressure.{36002} L-(−)-α-Methyldopa also improves trophoblast and endothelial cellular interactions in vitro.{36001}  

     

    Brand:
    Cayman
    SKU:21814 -

    Out of stock

  • L-(−)-α-Methyldopa is a dopamine (DOPA) decarboxylase inhibitor (ED50 = 21.8 mg/kg) and has antihypertensive activity in vitro and in vivo.{36001,36002,36000} L-(−)-α-Methyldopa enters the CNS and is metabolized to form α-methylnorepinephrine which acts as an agonist at α2-adrenergic receptors.{36001,36000} Formulations containing L-(−)-α-methyldopa are used to lower blood pressure.{36002} L-(−)-α-Methyldopa also improves trophoblast and endothelial cellular interactions in vitro.{36001}  

     

    Brand:
    Cayman
    SKU:21814 -

    Out of stock

  • L-(−)-α-Methyldopa is a dopamine (DOPA) decarboxylase inhibitor (ED50 = 21.8 mg/kg) and has antihypertensive activity in vitro and in vivo.{36001,36002,36000} L-(−)-α-Methyldopa enters the CNS and is metabolized to form α-methylnorepinephrine which acts as an agonist at α2-adrenergic receptors.{36001,36000} Formulations containing L-(−)-α-methyldopa are used to lower blood pressure.{36002} L-(−)-α-Methyldopa also improves trophoblast and endothelial cellular interactions in vitro.{36001}  

     

    Brand:
    Cayman
    SKU:21814 -

    Out of stock

  • L-006,235 is an orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM).{45555} It is selective for cathepsin K over cathepsins B, -L, and -S (Ki(app)s = 1, 6, and 47 µM, respectively). In an in vitro bone resorption assay, L-006,235 inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM). L-006,235 (10 mg/kg for 27 days) reduces the loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits compared to control animals.{45556} It also increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain when administered at a dose of 100 mg/kg.{45557}  

     

    Brand:
    Cayman
    SKU:28843 - 1 mg

    Available on backorder

  • L-006,235 is an orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM).{45555} It is selective for cathepsin K over cathepsins B, -L, and -S (Ki(app)s = 1, 6, and 47 µM, respectively). In an in vitro bone resorption assay, L-006,235 inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM). L-006,235 (10 mg/kg for 27 days) reduces the loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits compared to control animals.{45556} It also increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain when administered at a dose of 100 mg/kg.{45557}  

     

    Brand:
    Cayman
    SKU:28843 - 10 mg

    Available on backorder

  • L-006,235 is an orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM).{45555} It is selective for cathepsin K over cathepsins B, -L, and -S (Ki(app)s = 1, 6, and 47 µM, respectively). In an in vitro bone resorption assay, L-006,235 inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM). L-006,235 (10 mg/kg for 27 days) reduces the loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits compared to control animals.{45556} It also increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain when administered at a dose of 100 mg/kg.{45557}  

     

    Brand:
    Cayman
    SKU:28843 - 25 mg

    Available on backorder

  • L-006,235 is an orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM).{45555} It is selective for cathepsin K over cathepsins B, -L, and -S (Ki(app)s = 1, 6, and 47 µM, respectively). In an in vitro bone resorption assay, L-006,235 inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM). L-006,235 (10 mg/kg for 27 days) reduces the loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits compared to control animals.{45556} It also increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain when administered at a dose of 100 mg/kg.{45557}  

     

    Brand:
    Cayman
    SKU:28843 - 5 mg

    Available on backorder

  • L-156,602 is an antagonist of the complement component 5A (C5a) receptor (IC50 = 1.7 µg/L in a radioligand binding assay using neutrophil membranes).{38590} It is also a cyclic depsipeptide antibiotic that is active against Gram-positive bacteria.{38591} L-156,602 has anti-inflammatory activity in mice, decreasing inflammation induced by muramyl dipeptide (MDP) when administered at a dose of 0.5 mg/kg and by concanavalin A (Item No. 14951) at doses of 0.25 and 0.5 mg/kg.{38592}  

     

    Brand:
    Cayman
    SKU:23896 - 2.5 mg

    Available on backorder

  • L-156,602 is an antagonist of the complement component 5A (C5a) receptor (IC50 = 1.7 µg/L in a radioligand binding assay using neutrophil membranes).{38590} It is also a cyclic depsipeptide antibiotic that is active against Gram-positive bacteria.{38591} L-156,602 has anti-inflammatory activity in mice, decreasing inflammation induced by muramyl dipeptide (MDP) when administered at a dose of 0.5 mg/kg and by concanavalin A (Item No. 14951) at doses of 0.25 and 0.5 mg/kg.{38592}  

     

    Brand:
    Cayman
    SKU:23896 - 500 µg

    Available on backorder

  • Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).{1422} L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.{11629} L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats{11629} and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.{10774} At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.{16761}  

     

    Brand:
    Cayman
    SKU:10011565 - 1 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).{1422} L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.{11629} L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats{11629} and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.{10774} At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.{16761}  

     

    Brand:
    Cayman
    SKU:10011565 - 10 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).{1422} L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.{11629} L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats{11629} and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.{10774} At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.{16761}  

     

    Brand:
    Cayman
    SKU:10011565 - 5 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).{1422} L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.{11629} L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats{11629} and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.{10774} At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.{16761}  

     

    Brand:
    Cayman
    SKU:10011565 - 50 mg

    Available on backorder

  • L-165,041 is a potent and selective agonist of the nuclear receptor PPARβ/δ (Ki = 9 nM, EC50 = ~500 nM for hPPARβ/δ).{7166,10670} It is less effective against PPARα and PPARγ, with activity at those receptors depending on cell type and system of study.{10670,25703,25702} L-165,041 is used to evaluate the diverse roles of PPARβ/δ, including those related to cholesterol metabolism, inflammation, and neuroprotection.{10670,25701,25700}  

     

    Brand:
    Cayman
    SKU:9000249 - 10 mg

    Available on backorder

  • L-165,041 is a potent and selective agonist of the nuclear receptor PPARβ/δ (Ki = 9 nM, EC50 = ~500 nM for hPPARβ/δ).{7166,10670} It is less effective against PPARα and PPARγ, with activity at those receptors depending on cell type and system of study.{10670,25703,25702} L-165,041 is used to evaluate the diverse roles of PPARβ/δ, including those related to cholesterol metabolism, inflammation, and neuroprotection.{10670,25701,25700}  

     

    Brand:
    Cayman
    SKU:9000249 - 25 mg

    Available on backorder

  • L-165,041 is a potent and selective agonist of the nuclear receptor PPARβ/δ (Ki = 9 nM, EC50 = ~500 nM for hPPARβ/δ).{7166,10670} It is less effective against PPARα and PPARγ, with activity at those receptors depending on cell type and system of study.{10670,25703,25702} L-165,041 is used to evaluate the diverse roles of PPARβ/δ, including those related to cholesterol metabolism, inflammation, and neuroprotection.{10670,25701,25700}  

     

    Brand:
    Cayman
    SKU:9000249 - 5 mg

    Available on backorder

  • L-165,041 is a potent and selective agonist of the nuclear receptor PPARβ/δ (Ki = 9 nM, EC50 = ~500 nM for hPPARβ/δ).{7166,10670} It is less effective against PPARα and PPARγ, with activity at those receptors depending on cell type and system of study.{10670,25703,25702} L-165,041 is used to evaluate the diverse roles of PPARβ/δ, including those related to cholesterol metabolism, inflammation, and neuroprotection.{10670,25701,25700}  

     

    Brand:
    Cayman
    SKU:9000249 - 50 mg

    Available on backorder

  • L-368,899 is a non-peptide oxytocin receptor antagonist (IC50s = 8.9 and 26 nM in radioligand binding assays using isolated human and rat uterus, respectively).{53545} It is selective for oxytocin receptors over vasopressin V1a and V2 receptors (IC50s = 370 and 570 nM, respectively). L-368,899 reduces oxytocin-induced contraction of isolated rat uterus (pA2 = 8.9) and in situ rat uterus (ED50 = 0.35 mg/kg, i.v.).  

     

    Brand:
    Cayman
    SKU:29868 - 1 mg

    Available on backorder

  • L-368,899 is a non-peptide oxytocin receptor antagonist (IC50s = 8.9 and 26 nM in radioligand binding assays using isolated human and rat uterus, respectively).{53545} It is selective for oxytocin receptors over vasopressin V1a and V2 receptors (IC50s = 370 and 570 nM, respectively). L-368,899 reduces oxytocin-induced contraction of isolated rat uterus (pA2 = 8.9) and in situ rat uterus (ED50 = 0.35 mg/kg, i.v.).  

     

    Brand:
    Cayman
    SKU:29868 - 10 mg

    Available on backorder

  • L-368,899 is a non-peptide oxytocin receptor antagonist (IC50s = 8.9 and 26 nM in radioligand binding assays using isolated human and rat uterus, respectively).{53545} It is selective for oxytocin receptors over vasopressin V1a and V2 receptors (IC50s = 370 and 570 nM, respectively). L-368,899 reduces oxytocin-induced contraction of isolated rat uterus (pA2 = 8.9) and in situ rat uterus (ED50 = 0.35 mg/kg, i.v.).  

     

    Brand:
    Cayman
    SKU:29868 - 5 mg

    Available on backorder

  • The lipid mediator thromboxane (TX)A2 plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein-coupled receptor, referred to as the TXA2 receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.{14489} While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.{17467} L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM).{17468,1099} It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.{17468} Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.  

     

    Brand:
    Cayman
    SKU:10011562 - 1 mg

    Available on backorder

  • The lipid mediator thromboxane (TX)A2 plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein-coupled receptor, referred to as the TXA2 receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.{14489} While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.{17467} L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM).{17468,1099} It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.{17468} Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.  

     

    Brand:
    Cayman
    SKU:10011562 - 10 mg

    Available on backorder

  • The lipid mediator thromboxane (TX)A2 plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein-coupled receptor, referred to as the TXA2 receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.{14489} While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.{17467} L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM).{17468,1099} It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.{17468} Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.  

     

    Brand:
    Cayman
    SKU:10011562 - 25 mg

    Available on backorder

  • The lipid mediator thromboxane (TX)A2 plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein-coupled receptor, referred to as the TXA2 receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.{14489} While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.{17467} L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM).{17468,1099} It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.{17468} Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.  

     

    Brand:
    Cayman
    SKU:10011562 - 5 mg

    Available on backorder

  • L-655,708 is a ligand for α5 subunit-containing GABAA receptors that has nootropic activity.{56024} It selectively binds to α5 subunit-containing GABAA receptors over α1, α2, or α3 subunit-containing receptors (Kis = 1, 70, 48, and 31 nM, respectively, for recombinant human receptors). L-655,708 (10 nM) increases the amplitude of extracellular post-synaptic potentials (EPSPs) in mouse hippocampal slices. In vivo, L-655,708 (1.5 mg/animal) decreases the latency to find the platform and increases time spent in the target quadrant in the Morris water maze in mice.  

     

    Brand:
    Cayman
    SKU:30322 - 10 mg

    Available on backorder

  • L-655,708 is a ligand for α5 subunit-containing GABAA receptors that has nootropic activity.{56024} It selectively binds to α5 subunit-containing GABAA receptors over α1, α2, or α3 subunit-containing receptors (Kis = 1, 70, 48, and 31 nM, respectively, for recombinant human receptors). L-655,708 (10 nM) increases the amplitude of extracellular post-synaptic potentials (EPSPs) in mouse hippocampal slices. In vivo, L-655,708 (1.5 mg/animal) decreases the latency to find the platform and increases time spent in the target quadrant in the Morris water maze in mice.  

     

    Brand:
    Cayman
    SKU:30322 - 25 mg

    Available on backorder

  • L-655,708 is a ligand for α5 subunit-containing GABAA receptors that has nootropic activity.{56024} It selectively binds to α5 subunit-containing GABAA receptors over α1, α2, or α3 subunit-containing receptors (Kis = 1, 70, 48, and 31 nM, respectively, for recombinant human receptors). L-655,708 (10 nM) increases the amplitude of extracellular post-synaptic potentials (EPSPs) in mouse hippocampal slices. In vivo, L-655,708 (1.5 mg/animal) decreases the latency to find the platform and increases time spent in the target quadrant in the Morris water maze in mice.  

     

    Brand:
    Cayman
    SKU:30322 - 5 mg

    Available on backorder

  • L-655,708 is a ligand for α5 subunit-containing GABAA receptors that has nootropic activity.{56024} It selectively binds to α5 subunit-containing GABAA receptors over α1, α2, or α3 subunit-containing receptors (Kis = 1, 70, 48, and 31 nM, respectively, for recombinant human receptors). L-655,708 (10 nM) increases the amplitude of extracellular post-synaptic potentials (EPSPs) in mouse hippocampal slices. In vivo, L-655,708 (1.5 mg/animal) decreases the latency to find the platform and increases time spent in the target quadrant in the Morris water maze in mice.  

     

    Brand:
    Cayman
    SKU:30322 - 50 mg

    Available on backorder

  • L-685,458 is an inhibitor of γ-secretase (IC50 = 17 nM).{10285} It is selective for γ-secretase over HIV-1, cathepsin D, trypsin, HepC3 NS3, papain, and calpain I proteases (IC50s = >1,000 nM). L-685,458 inhibits production of amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) in Neuro2A cells transfected with human amyloid precursor protein (APP; IC50s = 402 and 775 nM, respectively). It is also an inhibitor of Notch signaling that blocks hypoxia-induced activity of the Notch-responsive reporters 12xCSL and CBF1 in isolated rat intervertebral disc cells.{35885}  

     

    Brand:
    Cayman
    SKU:-
  • L-685,458 is an inhibitor of γ-secretase (IC50 = 17 nM).{10285} It is selective for γ-secretase over HIV-1, cathepsin D, trypsin, HepC3 NS3, papain, and calpain I proteases (IC50s = >1,000 nM). L-685,458 inhibits production of amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) in Neuro2A cells transfected with human amyloid precursor protein (APP; IC50s = 402 and 775 nM, respectively). It is also an inhibitor of Notch signaling that blocks hypoxia-induced activity of the Notch-responsive reporters 12xCSL and CBF1 in isolated rat intervertebral disc cells.{35885}  

     

    Brand:
    Cayman
    SKU:-
  • L-685,458 is an inhibitor of γ-secretase (IC50 = 17 nM).{10285} It is selective for γ-secretase over HIV-1, cathepsin D, trypsin, HepC3 NS3, papain, and calpain I proteases (IC50s = >1,000 nM). L-685,458 inhibits production of amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) in Neuro2A cells transfected with human amyloid precursor protein (APP; IC50s = 402 and 775 nM, respectively). It is also an inhibitor of Notch signaling that blocks hypoxia-induced activity of the Notch-responsive reporters 12xCSL and CBF1 in isolated rat intervertebral disc cells.{35885}  

     

    Brand:
    Cayman
    SKU:-
  • L-701,324 is an NMDA receptor antagonist.{57099} It inhibits NMDA-induced currents in rat cortical neurons (Ki = 5.4 nM). L-701,324 inhibits seizures induced by N-methyl-DL-aspartate, pentylenetetrazole (PTZ; Item No. 18682), or electroshock, as well as audiogenic seizures in mice (ED50s = 3.5, 2.8, 1.4, and 0.96 mg/kg, respectively).{57100} It reduces the number of audiogenic seizures in a rat model of ethanol-induced withdrawal seizures when administered at a dose of 5 mg/kg.{57101} L-701,324 (2.5 and 5 mg/kg) reduces amphetamine-induced hyperactivity in rats.{57102}  

     

    Brand:
    Cayman
    SKU:30687 - 10 mg

    Available on backorder

  • L-701,324 is an NMDA receptor antagonist.{57099} It inhibits NMDA-induced currents in rat cortical neurons (Ki = 5.4 nM). L-701,324 inhibits seizures induced by N-methyl-DL-aspartate, pentylenetetrazole (PTZ; Item No. 18682), or electroshock, as well as audiogenic seizures in mice (ED50s = 3.5, 2.8, 1.4, and 0.96 mg/kg, respectively).{57100} It reduces the number of audiogenic seizures in a rat model of ethanol-induced withdrawal seizures when administered at a dose of 5 mg/kg.{57101} L-701,324 (2.5 and 5 mg/kg) reduces amphetamine-induced hyperactivity in rats.{57102}  

     

    Brand:
    Cayman
    SKU:30687 - 100 mg

    Available on backorder

  • L-701,324 is an NMDA receptor antagonist.{57099} It inhibits NMDA-induced currents in rat cortical neurons (Ki = 5.4 nM). L-701,324 inhibits seizures induced by N-methyl-DL-aspartate, pentylenetetrazole (PTZ; Item No. 18682), or electroshock, as well as audiogenic seizures in mice (ED50s = 3.5, 2.8, 1.4, and 0.96 mg/kg, respectively).{57100} It reduces the number of audiogenic seizures in a rat model of ethanol-induced withdrawal seizures when administered at a dose of 5 mg/kg.{57101} L-701,324 (2.5 and 5 mg/kg) reduces amphetamine-induced hyperactivity in rats.{57102}  

     

    Brand:
    Cayman
    SKU:30687 - 50 mg

    Available on backorder

  • L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).{57090} It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.{57091} It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).{57090} L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.{57092}  

     

    Brand:
    Cayman
    SKU:30894 - 10 mg

    Available on backorder

  • L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).{57090} It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.{57091} It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).{57090} L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.{57092}  

     

    Brand:
    Cayman
    SKU:30894 - 100 mg

    Available on backorder

  • L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).{57090} It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.{57091} It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).{57090} L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.{57092}  

     

    Brand:
    Cayman
    SKU:30894 - 5 mg

    Available on backorder

  • L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).{57090} It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.{57091} It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).{57090} L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.{57092}  

     

    Brand:
    Cayman
    SKU:30894 - 50 mg

    Available on backorder

  • L-741,626 is an antagonist of the dopamine D2 receptor (Kis = 2.4, 100, and 220 nM for human D2, D3, and D4, respectively, in a radioligand displacement assay).{38393} L-741,626 is selective for D2 receptors (Ki = 3.98 nM) over serotonin receptors (Kis ≤ 316.2 nM for human 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT3).{38397} In a functional assay, L-741,626 inhibits quinpirole-stimulated mitogenesis with EC50 values of 4.46 and 90.4 nM in CHO cells transfected with human D2long and D3 receptors, respectively.{38395} L-741,626 (3 μM) reversibly blocks D2-mediated currents in Xenopus oocytes via G protein-gated inwardly rectifying K+ (GIRK) channels.{38396} In models of potential antipsychotic activity, L-741,626 inhibits apomorphine-induced climbing behavior in mice (ID50 = 0.3 mg/kg, s.c.) and the conditioned avoidance response (CAR) in rats (ID50 = 6.1 mg/kg, s.c.).{38398} L-741,626 evokes a catalepsy response (AD50 = 7.0 mg/kg, s.c.) and blocks gnawing induced by methylphenidate (Item No. 11639; ID50 = 2.4 mg/kg, s.c.) in rat models of potential extrapyramidal activity.  

     

    Brand:
    Cayman
    SKU:22354 -

    Out of stock

  • L-741,626 is an antagonist of the dopamine D2 receptor (Kis = 2.4, 100, and 220 nM for human D2, D3, and D4, respectively, in a radioligand displacement assay).{38393} L-741,626 is selective for D2 receptors (Ki = 3.98 nM) over serotonin receptors (Kis ≤ 316.2 nM for human 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT3).{38397} In a functional assay, L-741,626 inhibits quinpirole-stimulated mitogenesis with EC50 values of 4.46 and 90.4 nM in CHO cells transfected with human D2long and D3 receptors, respectively.{38395} L-741,626 (3 μM) reversibly blocks D2-mediated currents in Xenopus oocytes via G protein-gated inwardly rectifying K+ (GIRK) channels.{38396} In models of potential antipsychotic activity, L-741,626 inhibits apomorphine-induced climbing behavior in mice (ID50 = 0.3 mg/kg, s.c.) and the conditioned avoidance response (CAR) in rats (ID50 = 6.1 mg/kg, s.c.).{38398} L-741,626 evokes a catalepsy response (AD50 = 7.0 mg/kg, s.c.) and blocks gnawing induced by methylphenidate (Item No. 11639; ID50 = 2.4 mg/kg, s.c.) in rat models of potential extrapyramidal activity.  

     

    Brand:
    Cayman
    SKU:22354 -

    Out of stock

  • L-741,626 is an antagonist of the dopamine D2 receptor (Kis = 2.4, 100, and 220 nM for human D2, D3, and D4, respectively, in a radioligand displacement assay).{38393} L-741,626 is selective for D2 receptors (Ki = 3.98 nM) over serotonin receptors (Kis ≤ 316.2 nM for human 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT3).{38397} In a functional assay, L-741,626 inhibits quinpirole-stimulated mitogenesis with EC50 values of 4.46 and 90.4 nM in CHO cells transfected with human D2long and D3 receptors, respectively.{38395} L-741,626 (3 μM) reversibly blocks D2-mediated currents in Xenopus oocytes via G protein-gated inwardly rectifying K+ (GIRK) channels.{38396} In models of potential antipsychotic activity, L-741,626 inhibits apomorphine-induced climbing behavior in mice (ID50 = 0.3 mg/kg, s.c.) and the conditioned avoidance response (CAR) in rats (ID50 = 6.1 mg/kg, s.c.).{38398} L-741,626 evokes a catalepsy response (AD50 = 7.0 mg/kg, s.c.) and blocks gnawing induced by methylphenidate (Item No. 11639; ID50 = 2.4 mg/kg, s.c.) in rat models of potential extrapyramidal activity.  

     

    Brand:
    Cayman
    SKU:22354 -

    Out of stock

  • L-748,337 is a β3-adrenergic receptor antagonist that displays selectivity over β1 and β2 receptors (Kis = 4, 390, and 204 nM, respectively).{32649} It has been shown to couple with Gi to activate MAPK signaling.{30080} L-748,337 can inhibit agonist-stimulated lipolysis in rhesus monkey adipocytes, as well as agonist-induced relaxation of smooth muscle.{32649}  

     

    Brand:
    Cayman
    SKU:19643 -

    Available on backorder

  • L-748,337 is a β3-adrenergic receptor antagonist that displays selectivity over β1 and β2 receptors (Kis = 4, 390, and 204 nM, respectively).{32649} It has been shown to couple with Gi to activate MAPK signaling.{30080} L-748,337 can inhibit agonist-stimulated lipolysis in rhesus monkey adipocytes, as well as agonist-induced relaxation of smooth muscle.{32649}  

     

    Brand:
    Cayman
    SKU:19643 -

    Available on backorder

  • L-748,337 is a β3-adrenergic receptor antagonist that displays selectivity over β1 and β2 receptors (Kis = 4, 390, and 204 nM, respectively).{32649} It has been shown to couple with Gi to activate MAPK signaling.{30080} L-748,337 can inhibit agonist-stimulated lipolysis in rhesus monkey adipocytes, as well as agonist-induced relaxation of smooth muscle.{32649}  

     

    Brand:
    Cayman
    SKU:19643 -

    Available on backorder

  • L-748,337 is a β3-adrenergic receptor antagonist that displays selectivity over β1 and β2 receptors (Kis = 4, 390, and 204 nM, respectively).{32649} It has been shown to couple with Gi to activate MAPK signaling.{30080} L-748,337 can inhibit agonist-stimulated lipolysis in rhesus monkey adipocytes, as well as agonist-induced relaxation of smooth muscle.{32649}  

     

    Brand:
    Cayman
    SKU:19643 -

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  • L-755,507 is a partial agonist of β3-adrenergic receptors (EC50 = 0.43 nM).{30079} It displays more than 440-fold selectivity for β3- over β1- and β2-adrenoceptors (EC50s = 580 and >10,000 nM, respectively).{30079} At 5 µM, this compound has been used to enhance CRISPR-mediated homology-directed repair efficiency by 3-fold for large fragment insertions and by 9-fold for point mutations.{30081} L-755,507 has been used to identify signaling pathways activated through β3-adrenergic receptors.{30080}  

     

    Brand:
    Cayman
    SKU:-

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  • L-755,507 is a partial agonist of β3-adrenergic receptors (EC50 = 0.43 nM).{30079} It displays more than 440-fold selectivity for β3- over β1- and β2-adrenoceptors (EC50s = 580 and >10,000 nM, respectively).{30079} At 5 µM, this compound has been used to enhance CRISPR-mediated homology-directed repair efficiency by 3-fold for large fragment insertions and by 9-fold for point mutations.{30081} L-755,507 has been used to identify signaling pathways activated through β3-adrenergic receptors.{30080}  

     

    Brand:
    Cayman
    SKU:-

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  • L-755,507 is a partial agonist of β3-adrenergic receptors (EC50 = 0.43 nM).{30079} It displays more than 440-fold selectivity for β3- over β1- and β2-adrenoceptors (EC50s = 580 and >10,000 nM, respectively).{30079} At 5 µM, this compound has been used to enhance CRISPR-mediated homology-directed repair efficiency by 3-fold for large fragment insertions and by 9-fold for point mutations.{30081} L-755,507 has been used to identify signaling pathways activated through β3-adrenergic receptors.{30080}  

     

    Brand:
    Cayman
    SKU:-

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  • L-755,507 is a partial agonist of β3-adrenergic receptors (EC50 = 0.43 nM).{30079} It displays more than 440-fold selectivity for β3- over β1- and β2-adrenoceptors (EC50s = 580 and >10,000 nM, respectively).{30079} At 5 µM, this compound has been used to enhance CRISPR-mediated homology-directed repair efficiency by 3-fold for large fragment insertions and by 9-fold for point mutations.{30081} L-755,507 has been used to identify signaling pathways activated through β3-adrenergic receptors.{30080}  

     

    Brand:
    Cayman
    SKU:-

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  • L-759,633 is a high-affinity peripheral cannabinoid receptor (CB2)-selective agonist with Ki values of 6.4 and 1,043 nM for CB2 and central cannabinoid (CB1) receptors, respectively. L-759,633 inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors with IC50 values of 8.1 nM and 10 µM, respectively.{13044}  

     

    Brand:
    Cayman
    SKU:10009280 - 1 mg

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  • L-759,633 is a high-affinity peripheral cannabinoid receptor (CB2)-selective agonist with Ki values of 6.4 and 1,043 nM for CB2 and central cannabinoid (CB1) receptors, respectively. L-759,633 inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors with IC50 values of 8.1 nM and 10 µM, respectively.{13044}  

     

    Brand:
    Cayman
    SKU:10009280 - 10 mg

    Available on backorder

  • L-759,633 is a high-affinity peripheral cannabinoid receptor (CB2)-selective agonist with Ki values of 6.4 and 1,043 nM for CB2 and central cannabinoid (CB1) receptors, respectively. L-759,633 inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors with IC50 values of 8.1 nM and 10 µM, respectively.{13044}  

     

    Brand:
    Cayman
    SKU:10009280 - 25 mg

    Available on backorder

  • L-759,633 is a high-affinity peripheral cannabinoid receptor (CB2)-selective agonist with Ki values of 6.4 and 1,043 nM for CB2 and central cannabinoid (CB1) receptors, respectively. L-759,633 inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors with IC50 values of 8.1 nM and 10 µM, respectively.{13044}  

     

    Brand:
    Cayman
    SKU:10009280 - 5 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:32504 - 10 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:32504 - 25 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:32504 - 5 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:32504 - 50 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and RAP1A in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein KI-RAS in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and RAP1A prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on KI-RAS prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:22940 - 10 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and RAP1A in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein KI-RAS in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and RAP1A prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on KI-RAS prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:22940 - 25 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and RAP1A in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein KI-RAS in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and RAP1A prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on KI-RAS prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:22940 - 5 mg

    Available on backorder

  • L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and RAP1A in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein KI-RAS in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and RAP1A prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on KI-RAS prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL-2 cells (IC50 = 0.81 μM).{41264}  

     

    Brand:
    Cayman
    SKU:22940 - 50 mg

    Available on backorder

  • L-779,450 is an ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that displays >7, >30, and >70-fold selectivity over p38α, GSK3β, and Lck, respectively.{31626} It has been shown to inhibit cell proliferation both in B-Raf mutated and wild-type melanoma cell lines, as well as to enhance tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in these cells.{31625}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • L-779,450 is an ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that displays >7, >30, and >70-fold selectivity over p38α, GSK3β, and Lck, respectively.{31626} It has been shown to inhibit cell proliferation both in B-Raf mutated and wild-type melanoma cell lines, as well as to enhance tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in these cells.{31625}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • L-779,450 is an ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that displays >7, >30, and >70-fold selectivity over p38α, GSK3β, and Lck, respectively.{31626} It has been shown to inhibit cell proliferation both in B-Raf mutated and wild-type melanoma cell lines, as well as to enhance tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in these cells.{31625}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • L-779,450 is an ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that displays >7, >30, and >70-fold selectivity over p38α, GSK3β, and Lck, respectively.{31626} It has been shown to inhibit cell proliferation both in B-Raf mutated and wild-type melanoma cell lines, as well as to enhance tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in these cells.{31625}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).{1422} L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.{9826} At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.{26175}  

     

    Brand:
    Cayman
    SKU:11129 - 1 mg

    Available on backorder

  • Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).{1422} L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.{9826} At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.{26175}  

     

    Brand:
    Cayman
    SKU:11129 - 10 mg

    Available on backorder

  • Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).{1422} L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.{9826} At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.{26175}  

     

    Brand:
    Cayman
    SKU:11129 - 5 mg

    Available on backorder

  • Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).{1422} L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.{9826} At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.{26175}  

     

    Brand:
    Cayman
    SKU:11129 - 50 mg

    Available on backorder