Chemicals
Showing 35251–35400 of 41137 results
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SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-328437 is a nonpeptide chemokine (C-C motif) receptor 3 (CCR3) antagonist (IC50 = 4.5 nM in a radioligand binding assay).{32621} It is selective for CCR3 over chemokine (C-X-C motif) receptor 1 (CXCR1), CXCR2, CCR7, complement 3a receptor (C3aR), and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively). SB-328437 (3.3-1,000 nM) inhibits calcium mobilization induced by chemokine (C-C motif) ligand 11 (CCL11), CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils. In vivo, SB-328437 reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in bronchoalveolar lavage fluid (BALF), and pulmonary IL-4 and TNF-α levels in a mouse model of asthma.{49498}
Brand:CaymanSKU:29677 - 1 mgAvailable on backorder
SB-328437 is a nonpeptide chemokine (C-C motif) receptor 3 (CCR3) antagonist (IC50 = 4.5 nM in a radioligand binding assay).{32621} It is selective for CCR3 over chemokine (C-X-C motif) receptor 1 (CXCR1), CXCR2, CCR7, complement 3a receptor (C3aR), and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively). SB-328437 (3.3-1,000 nM) inhibits calcium mobilization induced by chemokine (C-C motif) ligand 11 (CCL11), CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils. In vivo, SB-328437 reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in bronchoalveolar lavage fluid (BALF), and pulmonary IL-4 and TNF-α levels in a mouse model of asthma.{49498}
Brand:CaymanSKU:29677 - 10 mgAvailable on backorder
SB-328437 is a nonpeptide chemokine (C-C motif) receptor 3 (CCR3) antagonist (IC50 = 4.5 nM in a radioligand binding assay).{32621} It is selective for CCR3 over chemokine (C-X-C motif) receptor 1 (CXCR1), CXCR2, CCR7, complement 3a receptor (C3aR), and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively). SB-328437 (3.3-1,000 nM) inhibits calcium mobilization induced by chemokine (C-C motif) ligand 11 (CCL11), CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils. In vivo, SB-328437 reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in bronchoalveolar lavage fluid (BALF), and pulmonary IL-4 and TNF-α levels in a mouse model of asthma.{49498}
Brand:CaymanSKU:29677 - 5 mgAvailable on backorder
SB-334867 is an antagonist of the orexin 1 receptor (OX1R; KB = 39.8 nM) that is selective for OX1R over OX2R (KB = 1,995.3 nM).{43606} It reduces food intake and increases resting duration in rats, as well as inhibits orexin-A-induced increases in food intake, when administered at a dose of 30 mg/kg.{43607} SB-334867 (10 mg/kg) inhibits orexin-A-induced increases in grooming time in rats.{43606} It increases the seizure threshold in both the maximal electroshock seizure threshold (MEST) and 6 Hz psychomotor seizure test in mice when administered at doses of 30 and 3 mg/kg, respectively.{43608} Intracerebroventricular administration of SB-334867 (0.5-50 nmol) reduces morphine-induced analgesia in the formalin test in rats.{43609} SB-334867 (1.5 to 6 μg, intra-dentate gyrus injection) also reduces acquisition and consolidation of spatial memory in the Morris water maze in rats.{43610}
Brand:CaymanSKU:-Available on backorder
SB-334867 is an antagonist of the orexin 1 receptor (OX1R; KB = 39.8 nM) that is selective for OX1R over OX2R (KB = 1,995.3 nM).{43606} It reduces food intake and increases resting duration in rats, as well as inhibits orexin-A-induced increases in food intake, when administered at a dose of 30 mg/kg.{43607} SB-334867 (10 mg/kg) inhibits orexin-A-induced increases in grooming time in rats.{43606} It increases the seizure threshold in both the maximal electroshock seizure threshold (MEST) and 6 Hz psychomotor seizure test in mice when administered at doses of 30 and 3 mg/kg, respectively.{43608} Intracerebroventricular administration of SB-334867 (0.5-50 nmol) reduces morphine-induced analgesia in the formalin test in rats.{43609} SB-334867 (1.5 to 6 μg, intra-dentate gyrus injection) also reduces acquisition and consolidation of spatial memory in the Morris water maze in rats.{43610}
Brand:CaymanSKU:-Available on backorder
SB-334867 is an antagonist of the orexin 1 receptor (OX1R; KB = 39.8 nM) that is selective for OX1R over OX2R (KB = 1,995.3 nM).{43606} It reduces food intake and increases resting duration in rats, as well as inhibits orexin-A-induced increases in food intake, when administered at a dose of 30 mg/kg.{43607} SB-334867 (10 mg/kg) inhibits orexin-A-induced increases in grooming time in rats.{43606} It increases the seizure threshold in both the maximal electroshock seizure threshold (MEST) and 6 Hz psychomotor seizure test in mice when administered at doses of 30 and 3 mg/kg, respectively.{43608} Intracerebroventricular administration of SB-334867 (0.5-50 nmol) reduces morphine-induced analgesia in the formalin test in rats.{43609} SB-334867 (1.5 to 6 μg, intra-dentate gyrus injection) also reduces acquisition and consolidation of spatial memory in the Morris water maze in rats.{43610}
Brand:CaymanSKU:-Available on backorder
SB-334867 is an antagonist of the orexin 1 receptor (OX1R; KB = 39.8 nM) that is selective for OX1R over OX2R (KB = 1,995.3 nM).{43606} It reduces food intake and increases resting duration in rats, as well as inhibits orexin-A-induced increases in food intake, when administered at a dose of 30 mg/kg.{43607} SB-334867 (10 mg/kg) inhibits orexin-A-induced increases in grooming time in rats.{43606} It increases the seizure threshold in both the maximal electroshock seizure threshold (MEST) and 6 Hz psychomotor seizure test in mice when administered at doses of 30 and 3 mg/kg, respectively.{43608} Intracerebroventricular administration of SB-334867 (0.5-50 nmol) reduces morphine-induced analgesia in the formalin test in rats.{43609} SB-334867 (1.5 to 6 μg, intra-dentate gyrus injection) also reduces acquisition and consolidation of spatial memory in the Morris water maze in rats.{43610}
Brand:CaymanSKU:-Available on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research.{20043} In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 μM.{20043} A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain.{20044} Intrathecal pretreatment of 10 μl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration.{20045} Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.{20046}
Brand:CaymanSKU:11019 - 10 mgAvailable on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research.{20043} In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 μM.{20043} A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain.{20044} Intrathecal pretreatment of 10 μl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration.{20045} Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.{20046}
Brand:CaymanSKU:11019 - 25 mgAvailable on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research.{20043} In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 μM.{20043} A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain.{20044} Intrathecal pretreatment of 10 μl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration.{20045} Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.{20046}
Brand:CaymanSKU:11019 - 5 mgAvailable on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research.{20043} In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 μM.{20043} A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain.{20044} Intrathecal pretreatment of 10 μl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration.{20045} Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.{20046}
Brand:CaymanSKU:11019 - 50 mgAvailable on backorder
SB-3CT is a selective, mechanism-based inhibitor of the gelatinases, matrix metalloproteinase-2 (MMP-2) and MMP-9 (Kis = 28 and 400 nM, respectively).{26759,26757} First pass metabolism of SB-3CT in vivo produces a monohydroxylated metabolite that has greater inhibitory activity (Kis = 6 and 160 nM for MMP-2 and MMP-9, respectively).{26757} Both SB-3CT and its active metabolite can cross the blood-brain barrier and have utility in diseases of the central nervous system, such as stroke and traumatic brain injury.{26757,26758} SB-3CT may have applications in other pathologies involving gelatinases, including cancer, cardiovascular diseases, and inflammation.{26760,26756}
Brand:CaymanSKU:-Out of stock
SB-3CT is a selective, mechanism-based inhibitor of the gelatinases, matrix metalloproteinase-2 (MMP-2) and MMP-9 (Kis = 28 and 400 nM, respectively).{26759,26757} First pass metabolism of SB-3CT in vivo produces a monohydroxylated metabolite that has greater inhibitory activity (Kis = 6 and 160 nM for MMP-2 and MMP-9, respectively).{26757} Both SB-3CT and its active metabolite can cross the blood-brain barrier and have utility in diseases of the central nervous system, such as stroke and traumatic brain injury.{26757,26758} SB-3CT may have applications in other pathologies involving gelatinases, including cancer, cardiovascular diseases, and inflammation.{26760,26756}
Brand:CaymanSKU:-Out of stock
SB-3CT is a selective, mechanism-based inhibitor of the gelatinases, matrix metalloproteinase-2 (MMP-2) and MMP-9 (Kis = 28 and 400 nM, respectively).{26759,26757} First pass metabolism of SB-3CT in vivo produces a monohydroxylated metabolite that has greater inhibitory activity (Kis = 6 and 160 nM for MMP-2 and MMP-9, respectively).{26757} Both SB-3CT and its active metabolite can cross the blood-brain barrier and have utility in diseases of the central nervous system, such as stroke and traumatic brain injury.{26757,26758} SB-3CT may have applications in other pathologies involving gelatinases, including cancer, cardiovascular diseases, and inflammation.{26760,26756}
Brand:CaymanSKU:-Out of stock
SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}
Brand:CaymanSKU:22961 - 10 mgAvailable on backorder
SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}
Brand:CaymanSKU:22961 - 25 mgAvailable on backorder
SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}
Brand:CaymanSKU:22961 - 5 mgAvailable on backorder
SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}
Brand:CaymanSKU:22961 - 50 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors, and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis, and inflammation. SB-415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. {15623} As a result of GSK3 inhibition, SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM.{15623} SB-415286 also protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010247 - 1 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors, and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis, and inflammation. SB-415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. {15623} As a result of GSK3 inhibition, SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM.{15623} SB-415286 also protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010247 - 10 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors, and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis, and inflammation. SB-415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. {15623} As a result of GSK3 inhibition, SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM.{15623} SB-415286 also protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010247 - 5 mgAvailable on backorder
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.{21040} Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.{21040} In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.{21040}
Brand:CaymanSKU:11793 - 1 mgAvailable on backorder
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.{21040} Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.{21040} In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.{21040}
Brand:CaymanSKU:11793 - 10 mgAvailable on backorder
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.{21040} Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.{21040} In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.{21040}
Brand:CaymanSKU:11793 - 25 mgAvailable on backorder
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.{21040} Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.{21040} In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.{21040}
Brand:CaymanSKU:11793 - 5 mgAvailable on backorder
SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}
Brand:CaymanSKU:- SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}
Brand:CaymanSKU:- SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}
Brand:CaymanSKU:- SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}
Brand:CaymanSKU:-
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}
Brand:CaymanSKU:-Out of stock
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}
Brand:CaymanSKU:-Out of stock
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}
Brand:CaymanSKU:-Out of stock
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}
Brand:CaymanSKU:-Out of stock
SB-649868 is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 0.31 and 0.39 nM, respectively).{30229} In vivo, SB-649868 (3 and 10 mg/kg) decreases wakefulness and latency to fall asleep in rats.{46982} It also reduces binge eating of highly palatable food in a female rat model of stress-induced binge eating.
Brand:CaymanSKU:29477 - 1 mgAvailable on backorder
SB-649868 is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 0.31 and 0.39 nM, respectively).{30229} In vivo, SB-649868 (3 and 10 mg/kg) decreases wakefulness and latency to fall asleep in rats.{46982} It also reduces binge eating of highly palatable food in a female rat model of stress-induced binge eating.
Brand:CaymanSKU:29477 - 10 mgAvailable on backorder
SB-649868 is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 0.31 and 0.39 nM, respectively).{30229} In vivo, SB-649868 (3 and 10 mg/kg) decreases wakefulness and latency to fall asleep in rats.{46982} It also reduces binge eating of highly palatable food in a female rat model of stress-induced binge eating.
Brand:CaymanSKU:29477 - 25 mgAvailable on backorder
SB-649868 is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 0.31 and 0.39 nM, respectively).{30229} In vivo, SB-649868 (3 and 10 mg/kg) decreases wakefulness and latency to fall asleep in rats.{46982} It also reduces binge eating of highly palatable food in a female rat model of stress-induced binge eating.
Brand:CaymanSKU:29477 - 5 mgAvailable on backorder
SB-674042 is a potent and selective non-peptide orexin 1 receptor (OX1R) antagonist (Kd = 5.03 and 3.76 nM in whole cell binding and membrane-based assays, respectively).{34091} In calcium mobilization studies, it was >100-fold selective for OX1 over OX2 and did not show significant affinity for serotonergic, dopaminergic, adrenergic, or purinergic receptors at concentrations up to 10 µM.{34090}
Brand:CaymanSKU:21270 -Out of stock
SB-674042 is a potent and selective non-peptide orexin 1 receptor (OX1R) antagonist (Kd = 5.03 and 3.76 nM in whole cell binding and membrane-based assays, respectively).{34091} In calcium mobilization studies, it was >100-fold selective for OX1 over OX2 and did not show significant affinity for serotonergic, dopaminergic, adrenergic, or purinergic receptors at concentrations up to 10 µM.{34090}
Brand:CaymanSKU:21270 -Out of stock
SB-674042 is a potent and selective non-peptide orexin 1 receptor (OX1R) antagonist (Kd = 5.03 and 3.76 nM in whole cell binding and membrane-based assays, respectively).{34091} In calcium mobilization studies, it was >100-fold selective for OX1 over OX2 and did not show significant affinity for serotonergic, dopaminergic, adrenergic, or purinergic receptors at concentrations up to 10 µM.{34090}
Brand:CaymanSKU:21270 -Out of stock
SB-674042 is a potent and selective non-peptide orexin 1 receptor (OX1R) antagonist (Kd = 5.03 and 3.76 nM in whole cell binding and membrane-based assays, respectively).{34091} In calcium mobilization studies, it was >100-fold selective for OX1 over OX2 and did not show significant affinity for serotonergic, dopaminergic, adrenergic, or purinergic receptors at concentrations up to 10 µM.{34090}
Brand:CaymanSKU:21270 -Out of stock
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin (Item No. 92350). SB-705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated activation of TRPV1 receptors (pKis = 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively).{30459} It has been shown to induce rapid, reversible inhibition of capsaicin (IC50 = 3 nM)-, acid (pH 5.3)-, or heat (50°C; IC50 = 6 nM)-mediated activation of human TRPV1 (at -70 mV).{30459}
Brand:CaymanSKU:-Available on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin (Item No. 92350). SB-705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated activation of TRPV1 receptors (pKis = 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively).{30459} It has been shown to induce rapid, reversible inhibition of capsaicin (IC50 = 3 nM)-, acid (pH 5.3)-, or heat (50°C; IC50 = 6 nM)-mediated activation of human TRPV1 (at -70 mV).{30459}
Brand:CaymanSKU:-Available on backorder
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin (Item No. 92350). SB-705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated activation of TRPV1 receptors (pKis = 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively).{30459} It has been shown to induce rapid, reversible inhibition of capsaicin (IC50 = 3 nM)-, acid (pH 5.3)-, or heat (50°C; IC50 = 6 nM)-mediated activation of human TRPV1 (at -70 mV).{30459}
Brand:CaymanSKU:-Available on backorder
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).{40729,40731} SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.{40730} SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.{40731} In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.{40729} It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.{40732}
Brand:CaymanSKU:22200 -Out of stock
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).{40729,40731} SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.{40730} SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.{40731} In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.{40729} It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.{40732}
Brand:CaymanSKU:22200 -Out of stock
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).{40729,40731} SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.{40730} SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.{40731} In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.{40729} It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.{40732}
Brand:CaymanSKU:22200 -Out of stock
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).{40729,40731} SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.{40730} SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.{40731} In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.{40729} It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.{40732}
Brand:CaymanSKU:22200 -Out of stock
SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).{29618} It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.{37554} SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.{37555}
Brand:CaymanSKU:-Available on backorder
SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).{29618} It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.{37554} SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.{37555}
Brand:CaymanSKU:-Available on backorder
SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).{29618} It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.{37554} SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.{37555}
Brand:CaymanSKU:-Available on backorder
SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).{29618} It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.{37554} SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.{37555}
Brand:CaymanSKU:-Available on backorder
SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor).{45338} It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.
Brand:CaymanSKU:27998 - 10 mgAvailable on backorder
SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor).{45338} It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.
Brand:CaymanSKU:27998 - 100 mgAvailable on backorder
SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor).{45338} It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.
Brand:CaymanSKU:27998 - 50 mgAvailable on backorder
SB-772077B is a Rho-associated kinase (ROCK) inhibitor (IC50s = 5.6 and 6 nM for ROCK-I and ROCK-II, respectively).{16599} It is selective for ROCK-I and ROCK-II over Akt1, Akt2, and Akt3 (IC50s = 324, 1,950, and 1,290 nM, respectively), as well as Cdk2, GSK3α, IKKβ, JNK3, and Plk (IC50s = ≥7,000 nM for all), but also inhibits RSK1 and MSK1 (IC50s = 35 and 14 nM, respectively). SB-772077B inhibits LPS-induced TNF-α and IL-6 production in THP-1 cells in a concentration-dependent manner. It induces relaxation of pre-contracted isolated rat aortic rings (IC50 = 39 nM). It reduces blood pressure in spontaneously hypertensive rats in a dose-dependent manner and in DOCA-salt hypertensive rats when administered at a dose of 1 mg/kg. SB-772077B (30, 100, and 300 μg/kg, i.v.) reduces pulmonary and systemic arterial pressure and increases cardiac output in normotensive rats and rats with monocrotaline-induced pulmonary hypertension.{57163}
Brand:CaymanSKU:30975 - 1 mgAvailable on backorder
SB-772077B is a Rho-associated kinase (ROCK) inhibitor (IC50s = 5.6 and 6 nM for ROCK-I and ROCK-II, respectively).{16599} It is selective for ROCK-I and ROCK-II over Akt1, Akt2, and Akt3 (IC50s = 324, 1,950, and 1,290 nM, respectively), as well as Cdk2, GSK3α, IKKβ, JNK3, and Plk (IC50s = ≥7,000 nM for all), but also inhibits RSK1 and MSK1 (IC50s = 35 and 14 nM, respectively). SB-772077B inhibits LPS-induced TNF-α and IL-6 production in THP-1 cells in a concentration-dependent manner. It induces relaxation of pre-contracted isolated rat aortic rings (IC50 = 39 nM). It reduces blood pressure in spontaneously hypertensive rats in a dose-dependent manner and in DOCA-salt hypertensive rats when administered at a dose of 1 mg/kg. SB-772077B (30, 100, and 300 μg/kg, i.v.) reduces pulmonary and systemic arterial pressure and increases cardiac output in normotensive rats and rats with monocrotaline-induced pulmonary hypertension.{57163}
Brand:CaymanSKU:30975 - 5 mgAvailable on backorder
Inhibition of histone deacetylases (HDACs) leads to accumulation of acetylated histones, resulting in a variety of cell type-dependent responses including apoptosis, necrosis, differentiation, cell survival, inhibition of proliferation, and cytostasis. SB939 is an HDAC inhibitor that displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay and prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT116), and prostate cancer (PC-3) cell lines at IC50 values of 0.48, 0.56, 0.48, and 0.34 μM, respectively.{19767} SB939 is a pan-HDAC inhibitor binding all HDAC isozymes with similar affinity (Kis = 16-28 nM) with the exception of HDAC6 and 7 (Kis = 247 and 104 nM, respectively).{19767} SB939 demonstrates good bioavailability in vivo and significantly inhibits tumor growth in various xenograft mouse models at doses ranging from 25-100 mg/kg.{19767} It is being evaluated in phase I and phase II clinical trials in both hematological and solid tumor patients.{19767}
Brand:CaymanSKU:10443 - 1 mgAvailable on backorder
Inhibition of histone deacetylases (HDACs) leads to accumulation of acetylated histones, resulting in a variety of cell type-dependent responses including apoptosis, necrosis, differentiation, cell survival, inhibition of proliferation, and cytostasis. SB939 is an HDAC inhibitor that displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay and prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT116), and prostate cancer (PC-3) cell lines at IC50 values of 0.48, 0.56, 0.48, and 0.34 μM, respectively.{19767} SB939 is a pan-HDAC inhibitor binding all HDAC isozymes with similar affinity (Kis = 16-28 nM) with the exception of HDAC6 and 7 (Kis = 247 and 104 nM, respectively).{19767} SB939 demonstrates good bioavailability in vivo and significantly inhibits tumor growth in various xenograft mouse models at doses ranging from 25-100 mg/kg.{19767} It is being evaluated in phase I and phase II clinical trials in both hematological and solid tumor patients.{19767}
Brand:CaymanSKU:10443 - 10 mgAvailable on backorder
Inhibition of histone deacetylases (HDACs) leads to accumulation of acetylated histones, resulting in a variety of cell type-dependent responses including apoptosis, necrosis, differentiation, cell survival, inhibition of proliferation, and cytostasis. SB939 is an HDAC inhibitor that displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay and prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT116), and prostate cancer (PC-3) cell lines at IC50 values of 0.48, 0.56, 0.48, and 0.34 μM, respectively.{19767} SB939 is a pan-HDAC inhibitor binding all HDAC isozymes with similar affinity (Kis = 16-28 nM) with the exception of HDAC6 and 7 (Kis = 247 and 104 nM, respectively).{19767} SB939 demonstrates good bioavailability in vivo and significantly inhibits tumor growth in various xenograft mouse models at doses ranging from 25-100 mg/kg.{19767} It is being evaluated in phase I and phase II clinical trials in both hematological and solid tumor patients.{19767}
Brand:CaymanSKU:10443 - 25 mgAvailable on backorder
Inhibition of histone deacetylases (HDACs) leads to accumulation of acetylated histones, resulting in a variety of cell type-dependent responses including apoptosis, necrosis, differentiation, cell survival, inhibition of proliferation, and cytostasis. SB939 is an HDAC inhibitor that displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay and prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT116), and prostate cancer (PC-3) cell lines at IC50 values of 0.48, 0.56, 0.48, and 0.34 μM, respectively.{19767} SB939 is a pan-HDAC inhibitor binding all HDAC isozymes with similar affinity (Kis = 16-28 nM) with the exception of HDAC6 and 7 (Kis = 247 and 104 nM, respectively).{19767} SB939 demonstrates good bioavailability in vivo and significantly inhibits tumor growth in various xenograft mouse models at doses ranging from 25-100 mg/kg.{19767} It is being evaluated in phase I and phase II clinical trials in both hematological and solid tumor patients.{19767}
Brand:CaymanSKU:10443 - 5 mgAvailable on backorder
SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).{53726} It increases LDL receptor (LDLR) levels in HepG2 cells expressing PCSK9 when used at a concentration of 400 nM. SBC-110736 (8 mg/kg per day) reduces plasma total cholesterol levels by a mean of 38% in mice fed a high-fat diet. It also reduces plasma LDL cholesterol levels in mice fed a high-fat diet and exhibits an additive effect when administered in combination with atorvastatin (Item No. 10493).
Brand:CaymanSKU:23103 - 1 mgAvailable on backorder
SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).{53726} It increases LDL receptor (LDLR) levels in HepG2 cells expressing PCSK9 when used at a concentration of 400 nM. SBC-110736 (8 mg/kg per day) reduces plasma total cholesterol levels by a mean of 38% in mice fed a high-fat diet. It also reduces plasma LDL cholesterol levels in mice fed a high-fat diet and exhibits an additive effect when administered in combination with atorvastatin (Item No. 10493).
Brand:CaymanSKU:23103 - 10 mgAvailable on backorder
SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).{53726} It increases LDL receptor (LDLR) levels in HepG2 cells expressing PCSK9 when used at a concentration of 400 nM. SBC-110736 (8 mg/kg per day) reduces plasma total cholesterol levels by a mean of 38% in mice fed a high-fat diet. It also reduces plasma LDL cholesterol levels in mice fed a high-fat diet and exhibits an additive effect when administered in combination with atorvastatin (Item No. 10493).
Brand:CaymanSKU:23103 - 25 mgAvailable on backorder
SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).{53726} It increases LDL receptor (LDLR) levels in HepG2 cells expressing PCSK9 when used at a concentration of 400 nM. SBC-110736 (8 mg/kg per day) reduces plasma total cholesterol levels by a mean of 38% in mice fed a high-fat diet. It also reduces plasma LDL cholesterol levels in mice fed a high-fat diet and exhibits an additive effect when administered in combination with atorvastatin (Item No. 10493).
Brand:CaymanSKU:23103 - 5 mgAvailable on backorder
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with important roles in lipoprotein metabolism.{13178} PCSK9 overexpression in wild-type mice doubles plasma total cholesterol, possibly through acceleration of degradation of the LDL receptor (LDLR).{13178,13176} SBC-115076 is an inhibitor of PCSK9 action that blocks LDLR degradation in HEK293T cells expressing PCSK9.{30917} Through this mechanism, submicromolar concentrations of SBC-115076 increase the uptake of LDL by liver cells in vitro.{30917} SBC-115076 is effective in vivo, lowering cholesterol levels in mice that are fed a high fat diet.{30917}
Brand:CaymanSKU:-Available on backorder
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with important roles in lipoprotein metabolism.{13178} PCSK9 overexpression in wild-type mice doubles plasma total cholesterol, possibly through acceleration of degradation of the LDL receptor (LDLR).{13178,13176} SBC-115076 is an inhibitor of PCSK9 action that blocks LDLR degradation in HEK293T cells expressing PCSK9.{30917} Through this mechanism, submicromolar concentrations of SBC-115076 increase the uptake of LDL by liver cells in vitro.{30917} SBC-115076 is effective in vivo, lowering cholesterol levels in mice that are fed a high fat diet.{30917}
Brand:CaymanSKU:-Available on backorder
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with important roles in lipoprotein metabolism.{13178} PCSK9 overexpression in wild-type mice doubles plasma total cholesterol, possibly through acceleration of degradation of the LDL receptor (LDLR).{13178,13176} SBC-115076 is an inhibitor of PCSK9 action that blocks LDLR degradation in HEK293T cells expressing PCSK9.{30917} Through this mechanism, submicromolar concentrations of SBC-115076 increase the uptake of LDL by liver cells in vitro.{30917} SBC-115076 is effective in vivo, lowering cholesterol levels in mice that are fed a high fat diet.{30917}
Brand:CaymanSKU:-Available on backorder
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with important roles in lipoprotein metabolism.{13178} PCSK9 overexpression in wild-type mice doubles plasma total cholesterol, possibly through acceleration of degradation of the LDL receptor (LDLR).{13178,13176} SBC-115076 is an inhibitor of PCSK9 action that blocks LDLR degradation in HEK293T cells expressing PCSK9.{30917} Through this mechanism, submicromolar concentrations of SBC-115076 increase the uptake of LDL by liver cells in vitro.{30917} SBC-115076 is effective in vivo, lowering cholesterol levels in mice that are fed a high fat diet.{30917}
Brand:CaymanSKU:-Available on backorder
SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}
Brand:CaymanSKU:21241 -Out of stock
SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}
Brand:CaymanSKU:21241 -Out of stock
SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}
Brand:CaymanSKU:21241 -Out of stock
SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}
Brand:CaymanSKU:21241 -Out of stock
SBFI AM is a membrane-permeant, fluorescent Na+ indicator dye. It is selective for Na+ over K+ with Kd values of 20 and 120 mM for these ions, respectively.{30208} Increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.{30208} Therefore, ratio fluorometry and imaging can be performed with the same wavelengths. SBF AM is suitable for single intracellular dye injection and is typically used for high-resolution measurements of Na+ concentration in intact tissue through two-photon confocal imaging.{30207}
Brand:CaymanSKU:-Available on backorder
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}
Brand:CaymanSKU:-Available on backorder
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}
Brand:CaymanSKU:-Available on backorder
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}
Brand:CaymanSKU:-Available on backorder
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}
Brand:CaymanSKU:-Available on backorder