Chemicals
Showing 34501–34650 of 41137 results
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Ro 08-2750 is a p75 neurotrophin receptor (p75NTR) ligand that completely inhibits nerve growth factor (NGF) binding to p75NTR in PC12 cells when used at a concentration of 100 μM.{47722} It also binds to NGF dimers (Kd = ~1 μM) to induce a conformational change that prevents NGF binding to p75NTR or tropomyosin-related kinase A (TrkA). Ro 08-2750 inhibits NGF-induced death of SK-N-MC cells and inhibits autophosphorylation of TrkA in PC12 cells. It reverses NGF-induced decreases in β-catenin mRNA expression in, and migration of, SKOV3 and OVCAR-3 ovarian cancer cells.{47723}
Brand:CaymanSKU:28772 - 10 mgAvailable on backorder
Ro 08-2750 is a p75 neurotrophin receptor (p75NTR) ligand that completely inhibits nerve growth factor (NGF) binding to p75NTR in PC12 cells when used at a concentration of 100 μM.{47722} It also binds to NGF dimers (Kd = ~1 μM) to induce a conformational change that prevents NGF binding to p75NTR or tropomyosin-related kinase A (TrkA). Ro 08-2750 inhibits NGF-induced death of SK-N-MC cells and inhibits autophosphorylation of TrkA in PC12 cells. It reverses NGF-induced decreases in β-catenin mRNA expression in, and migration of, SKOV3 and OVCAR-3 ovarian cancer cells.{47723}
Brand:CaymanSKU:28772 - 5 mgAvailable on backorder
Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}
Brand:CaymanSKU:- Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}
Brand:CaymanSKU:- Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}
Brand:CaymanSKU:-
Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}
Brand:CaymanSKU:-Available on backorder
Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}
Brand:CaymanSKU:-Available on backorder
Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}
Brand:CaymanSKU:-Available on backorder
Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}
Brand:CaymanSKU:- Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}
Brand:CaymanSKU:- Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}
Brand:CaymanSKU:-
Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}
Brand:CaymanSKU:21669 -Out of stock
Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}
Brand:CaymanSKU:21669 -Out of stock
Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}
Brand:CaymanSKU:21669 -Out of stock
Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}
Brand:CaymanSKU:21669 -Out of stock
Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}
Brand:CaymanSKU:- Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}
Brand:CaymanSKU:- Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}
Brand:CaymanSKU:- Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}
Brand:CaymanSKU:-
Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}
Brand:CaymanSKU:29621 - 10 mgAvailable on backorder
Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}
Brand:CaymanSKU:29621 - 25 mgAvailable on backorder
Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}
Brand:CaymanSKU:29621 - 5 mgAvailable on backorder
Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}
Brand:CaymanSKU:10006415 - 10 mgAvailable on backorder
Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}
Brand:CaymanSKU:10006415 - 100 mgAvailable on backorder
Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}
Brand:CaymanSKU:10006415 - 5 mgAvailable on backorder
Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}
Brand:CaymanSKU:10006415 - 50 mgAvailable on backorder
Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}
Brand:CaymanSKU:19996 -Available on backorder
Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}
Brand:CaymanSKU:19996 -Available on backorder
Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}
Brand:CaymanSKU:19996 -Available on backorder
Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}
Brand:CaymanSKU:19996 -Available on backorder
Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}
Brand:CaymanSKU:29197 - 1 mgAvailable on backorder
Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}
Brand:CaymanSKU:29197 - 5 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 1 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 10 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 5 mgAvailable on backorder
The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:-
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 1 mgAvailable on backorder
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 10 mgAvailable on backorder
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 5 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 1 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 10 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 25 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 5 mgAvailable on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 10 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 25 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 5 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 50 mgAvailable on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 10 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 100 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 250 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 50 mgAvailable on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 1 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 10 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 25 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 5 mgAvailable on backorder
Sonic hedgehog (Shh) is the most widely characterized of the three vertebrate Hedgehog homologs, and is essential for proper embryonic development.{20489} Shh binds to its receptor, Patched (Ptch1), resulting in the de-repression of Smoothened.{3776,21773} This leads to the activation of Gli2, which regulates the transcription of target genes that include Gli1 and Ptch1. Robotnikinin is the first identified small molecule inhibitor of Shh signaling that acts upstream of Smo, binding directly to Shh with a Kd value of 3.1 μM.{16805,22122} Robotnikinin represses Gli-mediated transcription in primary human keratinocytes and synthetic human skin in a concentration-dependent manner.{16805}
Brand:CaymanSKU:-
Rocaglamide is an anti-inflammatory, insecticidal, and anticancer tetrahydrobenzofuran isolated from Aglaia species. It has been shown to inhibit both TNF-α and the activation of NF-κB in Jurkat T cells with IC50 values in the nanomolar range.{23675} At 25 nM, rocaglamide induces apoptosis in various human leukemia cell lines, activating p38 MAPK/JNK and suppressing ERK.{23676} Rocaglamide also reduces IFN-γ, TNF-α, IL-2, and IL-4 production in peripheral blood T cells at a concentration of 50 nM.{23677} Furthermore, rocaglamide can inhibit the T cell expression of the immune response transcription factor, nuclear factor of activated T cells.{23677}
Brand:CaymanSKU:- Rocaglamide is an anti-inflammatory, insecticidal, and anticancer tetrahydrobenzofuran isolated from Aglaia species. It has been shown to inhibit both TNF-α and the activation of NF-κB in Jurkat T cells with IC50 values in the nanomolar range.{23675} At 25 nM, rocaglamide induces apoptosis in various human leukemia cell lines, activating p38 MAPK/JNK and suppressing ERK.{23676} Rocaglamide also reduces IFN-γ, TNF-α, IL-2, and IL-4 production in peripheral blood T cells at a concentration of 50 nM.{23677} Furthermore, rocaglamide can inhibit the T cell expression of the immune response transcription factor, nuclear factor of activated T cells.{23677}
Brand:CaymanSKU:-
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.{53422,53423} It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 µg/ml for both).{53422} Roccellic acid (100 µg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.{53423}
Brand:CaymanSKU:29909 - 1 mgAvailable on backorder
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.{53422,53423} It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 µg/ml for both).{53422} Roccellic acid (100 µg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.{53423}
Brand:CaymanSKU:29909 - 5 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 10 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 25 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 5 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 50 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 100 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 250 mgAvailable on backorder