Chemicals
Showing 30451–30600 of 41137 results
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Ornidazole is an orally bioavailable 5-nitroimidazole derivative with antibacterial and antiprotozoal activities.{35717,26702} Ornidazole inhibits the growth of clinical isolates of B. fragilis (MICs = 0.5-5 μM) and various anaerobic bacteria when used at concentrations ranging from less than 0.1 to 3.2 μg/ml.{26702,48267} It also inhibits the growth of Giardia isolates (IC50s = 0.01-0.47 μg/ml).{48268} Oral administration of ornidazole reduces T. vaginalis and T. foetus infection in mice and E. histolytica infection in rats with curative dose (CD50) values of 37, 3, and 10 mg/kg, respectively.{35717} Ornidazole (400 mg/kg per day) induces infertility in male rats within 7 days and inhibits spermatozoa binding to rat oocyte zona pellucida.{48269,48270}
Brand:CaymanSKU:26818 - 50 gAvailable on backorder
Oroxylin A is a flavonoid that has been found in S. radix and has diverse biological activities.{47464,47465,47466} It inhibits decreases in cell viability and increases in nitric oxide (NO) production induced by polyinosinic-polycytidylic acid (poly(I:C)) in RAW 264.7 macrophages when used at concentrations ranging from 5 to 25 μM.{47465} Oroxylin A (10-50 μM) also inhibits poly(I:C)-induced increases in IL-1α, IL-1β, GM-CSF, IL-6, IL-10, monocyte chemoattractant protein-1 (MCP-1), and TNF-α production in RAW 264.7 cells. Oroxylin A (10 and 20 μM) inhibits hypoxia-induced migration and invasion of MCF-7, DU145, and HepG2 cells in wound healing and cell invasion assays, respectively.{47466} It is an inhibitor of the UDP-glucuronosyltransferase (UGT) isoform UGT1A1 (IC50 = 9.14 μM) and P-glycoprotein (IC50 = 78.3 μM).{47467,47468} Oroxylin A increases the cytotoxicity of the P-glycoprotein substrate paraquat in MDR1-MDCKII cells and paclitaxel (Item No. 10461) in MX-1 and MX-1/T cells.{47468}
Brand:CaymanSKU:27363 - 1 mgAvailable on backorder
Oroxylin A is a flavonoid that has been found in S. radix and has diverse biological activities.{47464,47465,47466} It inhibits decreases in cell viability and increases in nitric oxide (NO) production induced by polyinosinic-polycytidylic acid (poly(I:C)) in RAW 264.7 macrophages when used at concentrations ranging from 5 to 25 μM.{47465} Oroxylin A (10-50 μM) also inhibits poly(I:C)-induced increases in IL-1α, IL-1β, GM-CSF, IL-6, IL-10, monocyte chemoattractant protein-1 (MCP-1), and TNF-α production in RAW 264.7 cells. Oroxylin A (10 and 20 μM) inhibits hypoxia-induced migration and invasion of MCF-7, DU145, and HepG2 cells in wound healing and cell invasion assays, respectively.{47466} It is an inhibitor of the UDP-glucuronosyltransferase (UGT) isoform UGT1A1 (IC50 = 9.14 μM) and P-glycoprotein (IC50 = 78.3 μM).{47467,47468} Oroxylin A increases the cytotoxicity of the P-glycoprotein substrate paraquat in MDR1-MDCKII cells and paclitaxel (Item No. 10461) in MX-1 and MX-1/T cells.{47468}
Brand:CaymanSKU:27363 - 10 mgAvailable on backorder
Oroxylin A is a flavonoid that has been found in S. radix and has diverse biological activities.{47464,47465,47466} It inhibits decreases in cell viability and increases in nitric oxide (NO) production induced by polyinosinic-polycytidylic acid (poly(I:C)) in RAW 264.7 macrophages when used at concentrations ranging from 5 to 25 μM.{47465} Oroxylin A (10-50 μM) also inhibits poly(I:C)-induced increases in IL-1α, IL-1β, GM-CSF, IL-6, IL-10, monocyte chemoattractant protein-1 (MCP-1), and TNF-α production in RAW 264.7 cells. Oroxylin A (10 and 20 μM) inhibits hypoxia-induced migration and invasion of MCF-7, DU145, and HepG2 cells in wound healing and cell invasion assays, respectively.{47466} It is an inhibitor of the UDP-glucuronosyltransferase (UGT) isoform UGT1A1 (IC50 = 9.14 μM) and P-glycoprotein (IC50 = 78.3 μM).{47467,47468} Oroxylin A increases the cytotoxicity of the P-glycoprotein substrate paraquat in MDR1-MDCKII cells and paclitaxel (Item No. 10461) in MX-1 and MX-1/T cells.{47468}
Brand:CaymanSKU:27363 - 25 mgAvailable on backorder
Oroxylin A is a flavonoid that has been found in S. radix and has diverse biological activities.{47464,47465,47466} It inhibits decreases in cell viability and increases in nitric oxide (NO) production induced by polyinosinic-polycytidylic acid (poly(I:C)) in RAW 264.7 macrophages when used at concentrations ranging from 5 to 25 μM.{47465} Oroxylin A (10-50 μM) also inhibits poly(I:C)-induced increases in IL-1α, IL-1β, GM-CSF, IL-6, IL-10, monocyte chemoattractant protein-1 (MCP-1), and TNF-α production in RAW 264.7 cells. Oroxylin A (10 and 20 μM) inhibits hypoxia-induced migration and invasion of MCF-7, DU145, and HepG2 cells in wound healing and cell invasion assays, respectively.{47466} It is an inhibitor of the UDP-glucuronosyltransferase (UGT) isoform UGT1A1 (IC50 = 9.14 μM) and P-glycoprotein (IC50 = 78.3 μM).{47467,47468} Oroxylin A increases the cytotoxicity of the P-glycoprotein substrate paraquat in MDR1-MDCKII cells and paclitaxel (Item No. 10461) in MX-1 and MX-1/T cells.{47468}
Brand:CaymanSKU:27363 - 5 mgAvailable on backorder
Orphenadrine is a muscarinic acetylcholine receptor (mAChR) antagonist (Kds = 48, 213, 120, 170, and 129 nM for M1-M5 receptors, respectively).{25806} Orphenadrine (2-5 mg/kg, i.v.) decreases muscle activity induced by the mAChR agonist oxotremorine in rabbits.{47476} It is also an NMDA receptor antagonist with a Ki value of 6 µM in a radioligand binding assay in human postmortem frontal cortex and an IC50 value of 16.2 µM for inhibiting steady state currents in cultured superior colliculus neurons.{47475} Formulations containing orphenadrine have been used in the treatment of acute painful musculoskeletal conditions, including muscle spasms.
Brand:CaymanSKU:26391 - 10 mgAvailable on backorder
Orphenadrine is a muscarinic acetylcholine receptor (mAChR) antagonist (Kds = 48, 213, 120, 170, and 129 nM for M1-M5 receptors, respectively).{25806} Orphenadrine (2-5 mg/kg, i.v.) decreases muscle activity induced by the mAChR agonist oxotremorine in rabbits.{47476} It is also an NMDA receptor antagonist with a Ki value of 6 µM in a radioligand binding assay in human postmortem frontal cortex and an IC50 value of 16.2 µM for inhibiting steady state currents in cultured superior colliculus neurons.{47475} Formulations containing orphenadrine have been used in the treatment of acute painful musculoskeletal conditions, including muscle spasms.
Brand:CaymanSKU:26391 - 25 mgAvailable on backorder
Orphenadrine is a muscarinic acetylcholine receptor (mAChR) antagonist (Kds = 48, 213, 120, 170, and 129 nM for M1-M5 receptors, respectively).{25806} Orphenadrine (2-5 mg/kg, i.v.) decreases muscle activity induced by the mAChR agonist oxotremorine in rabbits.{47476} It is also an NMDA receptor antagonist with a Ki value of 6 µM in a radioligand binding assay in human postmortem frontal cortex and an IC50 value of 16.2 µM for inhibiting steady state currents in cultured superior colliculus neurons.{47475} Formulations containing orphenadrine have been used in the treatment of acute painful musculoskeletal conditions, including muscle spasms.
Brand:CaymanSKU:26391 - 50 mgAvailable on backorder
Orsellinic acid is a fungal metabolite and benzoic acid derivative with antioxidant and neuroprotective activities.{43371,43459} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 5 mM.{43371} Orsellinic acid (1 μg/ml) prevents PARP cleavage induced by platelet-activating factor (PAF) in PC12-AC cells and PAF-induced cytotoxicity in PAF receptor null (Pafr-/-) mouse cerebellar granule cells.{43459}
Brand:CaymanSKU:22708 -Out of stock
Orsellinic acid is a fungal metabolite and benzoic acid derivative with antioxidant and neuroprotective activities.{43371,43459} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 5 mM.{43371} Orsellinic acid (1 μg/ml) prevents PARP cleavage induced by platelet-activating factor (PAF) in PC12-AC cells and PAF-induced cytotoxicity in PAF receptor null (Pafr-/-) mouse cerebellar granule cells.{43459}
Brand:CaymanSKU:22708 -Out of stock
Orsellinic acid is a fungal metabolite and benzoic acid derivative with antioxidant and neuroprotective activities.{43371,43459} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 5 mM.{43371} Orsellinic acid (1 μg/ml) prevents PARP cleavage induced by platelet-activating factor (PAF) in PC12-AC cells and PAF-induced cytotoxicity in PAF receptor null (Pafr-/-) mouse cerebellar granule cells.{43459}
Brand:CaymanSKU:22708 -Out of stock
Orsellinic acid is a fungal metabolite and benzoic acid derivative with antioxidant and neuroprotective activities.{43371,43459} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals with an IC50 value of 5 mM.{43371} Orsellinic acid (1 μg/ml) prevents PARP cleavage induced by platelet-activating factor (PAF) in PC12-AC cells and PAF-induced cytotoxicity in PAF receptor null (Pafr-/-) mouse cerebellar granule cells.{43459}
Brand:CaymanSKU:22708 -Out of stock
Orteronel is a non-steroidal inhibitor of the 17,20-lyase activity of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 48 and 19 nM for the rat and human enzyme, respectively), which is the CYP17A1 activity that converts progestogens into androgens.{39593} Orteronel is selective for the 17,20-lyase activity of CYP17A1 over its 11-hydroxylase activity and CYP3A4 (IC50s = >1,000 and >10,000 nM, respectively). It decreases adrenocorticotropic hormone-induced production of DHEA, androstenedione, cortisol, and aldosterone in monkey adrenal cells (IC50s = 110, 130, 310, and 4,400 nmol/L, respectively) and inhibits DHEA production in NCI-H295R human adrenocortical tumor cells.{39594} A single oral dose of orteronel (0.3-10 mg/kg) dose-dependently decreases DHEA, cortisol, and testosterone levels in the plasma of intact cynomolgus monkeys for at least 10 hours, and chronic dosing of 15 mg/kg twice daily suppresses levels for up to seven days of treatment. It also decreases DHEA and testosterone plasma levels in castrated monkeys, indicating an effect on extra-gonadal production of testosterone.
Brand:CaymanSKU:24191 - 10 mgAvailable on backorder
Orteronel is a non-steroidal inhibitor of the 17,20-lyase activity of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 48 and 19 nM for the rat and human enzyme, respectively), which is the CYP17A1 activity that converts progestogens into androgens.{39593} Orteronel is selective for the 17,20-lyase activity of CYP17A1 over its 11-hydroxylase activity and CYP3A4 (IC50s = >1,000 and >10,000 nM, respectively). It decreases adrenocorticotropic hormone-induced production of DHEA, androstenedione, cortisol, and aldosterone in monkey adrenal cells (IC50s = 110, 130, 310, and 4,400 nmol/L, respectively) and inhibits DHEA production in NCI-H295R human adrenocortical tumor cells.{39594} A single oral dose of orteronel (0.3-10 mg/kg) dose-dependently decreases DHEA, cortisol, and testosterone levels in the plasma of intact cynomolgus monkeys for at least 10 hours, and chronic dosing of 15 mg/kg twice daily suppresses levels for up to seven days of treatment. It also decreases DHEA and testosterone plasma levels in castrated monkeys, indicating an effect on extra-gonadal production of testosterone.
Brand:CaymanSKU:24191 - 25 mgAvailable on backorder
Orteronel is a non-steroidal inhibitor of the 17,20-lyase activity of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 48 and 19 nM for the rat and human enzyme, respectively), which is the CYP17A1 activity that converts progestogens into androgens.{39593} Orteronel is selective for the 17,20-lyase activity of CYP17A1 over its 11-hydroxylase activity and CYP3A4 (IC50s = >1,000 and >10,000 nM, respectively). It decreases adrenocorticotropic hormone-induced production of DHEA, androstenedione, cortisol, and aldosterone in monkey adrenal cells (IC50s = 110, 130, 310, and 4,400 nmol/L, respectively) and inhibits DHEA production in NCI-H295R human adrenocortical tumor cells.{39594} A single oral dose of orteronel (0.3-10 mg/kg) dose-dependently decreases DHEA, cortisol, and testosterone levels in the plasma of intact cynomolgus monkeys for at least 10 hours, and chronic dosing of 15 mg/kg twice daily suppresses levels for up to seven days of treatment. It also decreases DHEA and testosterone plasma levels in castrated monkeys, indicating an effect on extra-gonadal production of testosterone.
Brand:CaymanSKU:24191 - 5 mgAvailable on backorder
ortho-fluoro 4-ANBP (Item No. 25958) is an analytical reference standard that is structurally similar to known opioids. It is an intermediate in the synthesis of N-benzyl ortho-fluoro norfentanyl (Item No. 25540). This product is intended for research and forensic applications.
Brand:CaymanSKU:25958 - 1 mgAvailable on backorder
ortho-fluoro 4-ANBP (Item No. 25958) is an analytical reference standard that is structurally similar to known opioids. It is an intermediate in the synthesis of N-benzyl ortho-fluoro norfentanyl (Item No. 25540). This product is intended for research and forensic applications.
Brand:CaymanSKU:25958 - 5 mgAvailable on backorder
Lysine-specific demethylase 1 (LSD1) demethylates H3K4 and H3K9, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} ORY-1001 is an orally available, selective inhibitor of LSD1 (IC50 < 20 nM).{31138,31139} It targets acute myeloid leukemia (AML) stem cells and significantly reduces tumor cell load while increasing survival time in mouse models of AML.{31138,31139} ORY-1001 is in clinical trials for cancer treatment.{31139}
Brand:CaymanSKU:-Available on backorder
Lysine-specific demethylase 1 (LSD1) demethylates H3K4 and H3K9, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} ORY-1001 is an orally available, selective inhibitor of LSD1 (IC50 < 20 nM).{31138,31139} It targets acute myeloid leukemia (AML) stem cells and significantly reduces tumor cell load while increasing survival time in mouse models of AML.{31138,31139} ORY-1001 is in clinical trials for cancer treatment.{31139}
Brand:CaymanSKU:-Available on backorder
Lysine-specific demethylase 1 (LSD1) demethylates H3K4 and H3K9, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} ORY-1001 is an orally available, selective inhibitor of LSD1 (IC50 < 20 nM).{31138,31139} It targets acute myeloid leukemia (AML) stem cells and significantly reduces tumor cell load while increasing survival time in mouse models of AML.{31138,31139} ORY-1001 is in clinical trials for cancer treatment.{31139}
Brand:CaymanSKU:-Available on backorder
Lysine-specific demethylase 1 (LSD1) demethylates H3K4 and H3K9, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} ORY-1001 is an orally available, selective inhibitor of LSD1 (IC50 < 20 nM).{31138,31139} It targets acute myeloid leukemia (AML) stem cells and significantly reduces tumor cell load while increasing survival time in mouse models of AML.{31138,31139} ORY-1001 is in clinical trials for cancer treatment.{31139}
Brand:CaymanSKU:-Available on backorder
Oseltamivir is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Once hydrolyzed in the liver to its active metabolite, oseltamivir acid (Item No. 15779), it can competitively inhibit viral neuraminidase (IC50s = 0.1-4.9 nM for influenza neuraminidases A and B), blocking the release of new viral particles from a host cell.{25825,25826,25830,25829,25828}
Brand:CaymanSKU:- Oseltamivir is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Once hydrolyzed in the liver to its active metabolite, oseltamivir acid (Item No. 15779), it can competitively inhibit viral neuraminidase (IC50s = 0.1-4.9 nM for influenza neuraminidases A and B), blocking the release of new viral particles from a host cell.{25825,25826,25830,25829,25828}
Brand:CaymanSKU:- Oseltamivir is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Once hydrolyzed in the liver to its active metabolite, oseltamivir acid (Item No. 15779), it can competitively inhibit viral neuraminidase (IC50s = 0.1-4.9 nM for influenza neuraminidases A and B), blocking the release of new viral particles from a host cell.{25825,25826,25830,25829,25828}
Brand:CaymanSKU:-
Oseltamivir (GS-4104) is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Oseltamivir acid is the active metabolite of oseltamivir.{25825,25826} It acts as an inhibitor of influenza neuraminidases A and B (IC50 = 0.1 to 4.9 nM for both enzymes), in this way preventing virus budding and release.{25830,25829,25828}
Brand:CaymanSKU:- Oseltamivir (GS-4104) is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Oseltamivir acid is the active metabolite of oseltamivir.{25825,25826} It acts as an inhibitor of influenza neuraminidases A and B (IC50 = 0.1 to 4.9 nM for both enzymes), in this way preventing virus budding and release.{25830,25829,25828}
Brand:CaymanSKU:- Oseltamivir (GS-4104) is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Oseltamivir acid is the active metabolite of oseltamivir.{25825,25826} It acts as an inhibitor of influenza neuraminidases A and B (IC50 = 0.1 to 4.9 nM for both enzymes), in this way preventing virus budding and release.{25830,25829,25828}
Brand:CaymanSKU:- Oseltamivir (GS-4104) is an antiviral prodrug targeted against the influenza viruses.{25827,25824} Oseltamivir acid is the active metabolite of oseltamivir.{25825,25826} It acts as an inhibitor of influenza neuraminidases A and B (IC50 = 0.1 to 4.9 nM for both enzymes), in this way preventing virus budding and release.{25830,25829,25828}
Brand:CaymanSKU:-
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).{29740,29741} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.{29741} OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.{29740,29742,29743} OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.{29741,29739}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).{29740,29741} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.{29741} OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.{29740,29742,29743} OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.{29741,29739}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).{29740,29741} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.{29741} OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.{29740,29742,29743} OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.{29741,29739}
Brand:CaymanSKU:-Available on backorder
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).{29740,29741} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.{29741} OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.{29740,29742,29743} OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.{29741,29739}
Brand:CaymanSKU:-Available on backorder
OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively). OSI-930 inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active V560G mutation (KitV560G), respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively). It also inhibits VEGF-induced autophosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50 = 64.4 nM). OSI-930 (100 nM) decreases endothelial sprout formation by greater than 50% in isolated rat aortic rings. It reduces tumor growth in a variety of mouse xenograft models, including colon and small-cell lung cancer, melanoma, and glioblastoma models, when administered orally at a dose of 200 mg/kg per day.
Brand:CaymanSKU:29379 - 10 mgAvailable on backorder
OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively). OSI-930 inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active V560G mutation (KitV560G), respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively). It also inhibits VEGF-induced autophosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50 = 64.4 nM). OSI-930 (100 nM) decreases endothelial sprout formation by greater than 50% in isolated rat aortic rings. It reduces tumor growth in a variety of mouse xenograft models, including colon and small-cell lung cancer, melanoma, and glioblastoma models, when administered orally at a dose of 200 mg/kg per day.
Brand:CaymanSKU:29379 - 25 mgAvailable on backorder
OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively). OSI-930 inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active V560G mutation (KitV560G), respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively). It also inhibits VEGF-induced autophosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50 = 64.4 nM). OSI-930 (100 nM) decreases endothelial sprout formation by greater than 50% in isolated rat aortic rings. It reduces tumor growth in a variety of mouse xenograft models, including colon and small-cell lung cancer, melanoma, and glioblastoma models, when administered orally at a dose of 200 mg/kg per day.
Brand:CaymanSKU:29379 - 5 mgAvailable on backorder
OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively). OSI-930 inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active V560G mutation (KitV560G), respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively). It also inhibits VEGF-induced autophosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50 = 64.4 nM). OSI-930 (100 nM) decreases endothelial sprout formation by greater than 50% in isolated rat aortic rings. It reduces tumor growth in a variety of mouse xenograft models, including colon and small-cell lung cancer, melanoma, and glioblastoma models, when administered orally at a dose of 200 mg/kg per day.
Brand:CaymanSKU:29379 - 50 mgAvailable on backorder
OSMI-1 is a quinolinone-6-sulfonamide that inhibits O-GlcNAc transferase (OGT; IC50 = 2.7 μM) in vitro.{39059} It is cell permeable and inhibits global O-GlcNAcylation in a dose-dependent manner in CHO cells. OSMI-1 induces a mass shift of nucleoporin62 (Nup62) that corresponds to the loss of O-GlcNAc residues and decreases levels of cellular O-GlcNAcase (OGA). OSMI-1 (50 μM) also causes a 50% decrease in CHO cell viability after 24 hours.
Brand:CaymanSKU:21894 -Out of stock
OSMI-1 is a quinolinone-6-sulfonamide that inhibits O-GlcNAc transferase (OGT; IC50 = 2.7 μM) in vitro.{39059} It is cell permeable and inhibits global O-GlcNAcylation in a dose-dependent manner in CHO cells. OSMI-1 induces a mass shift of nucleoporin62 (Nup62) that corresponds to the loss of O-GlcNAc residues and decreases levels of cellular O-GlcNAcase (OGA). OSMI-1 (50 μM) also causes a 50% decrease in CHO cell viability after 24 hours.
Brand:CaymanSKU:21894 -Out of stock
OSMI-1 is a quinolinone-6-sulfonamide that inhibits O-GlcNAc transferase (OGT; IC50 = 2.7 μM) in vitro.{39059} It is cell permeable and inhibits global O-GlcNAcylation in a dose-dependent manner in CHO cells. OSMI-1 induces a mass shift of nucleoporin62 (Nup62) that corresponds to the loss of O-GlcNAc residues and decreases levels of cellular O-GlcNAcase (OGA). OSMI-1 (50 μM) also causes a 50% decrease in CHO cell viability after 24 hours.
Brand:CaymanSKU:21894 -Out of stock
OSMI-1 is a quinolinone-6-sulfonamide that inhibits O-GlcNAc transferase (OGT; IC50 = 2.7 μM) in vitro.{39059} It is cell permeable and inhibits global O-GlcNAcylation in a dose-dependent manner in CHO cells. OSMI-1 induces a mass shift of nucleoporin62 (Nup62) that corresponds to the loss of O-GlcNAc residues and decreases levels of cellular O-GlcNAcase (OGA). OSMI-1 (50 μM) also causes a 50% decrease in CHO cell viability after 24 hours.
Brand:CaymanSKU:21894 -Out of stock
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM) that binds to the estrogen receptors ERα and ERβ (Kis = 380 and 410 nM, respectively).{41365} It increases vaginal weight and vaginal epithelial height (ED50s = 0.48 and 0.39 mg/kg per day, respectively) in an ovariectomized rat model of menopause. Ospemifene also upregulates progesterone receptors in vaginal epithelium and stroma and inhibits estrogen response element-induced transactivation in MCF-7 cells. Formulations containing ospemifene have been used to treat vulvar and vaginal atrophy-induced dyspareunia.
Brand:CaymanSKU:23755 - 100 mgAvailable on backorder
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM) that binds to the estrogen receptors ERα and ERβ (Kis = 380 and 410 nM, respectively).{41365} It increases vaginal weight and vaginal epithelial height (ED50s = 0.48 and 0.39 mg/kg per day, respectively) in an ovariectomized rat model of menopause. Ospemifene also upregulates progesterone receptors in vaginal epithelium and stroma and inhibits estrogen response element-induced transactivation in MCF-7 cells. Formulations containing ospemifene have been used to treat vulvar and vaginal atrophy-induced dyspareunia.
Brand:CaymanSKU:23755 - 250 mgAvailable on backorder
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM) that binds to the estrogen receptors ERα and ERβ (Kis = 380 and 410 nM, respectively).{41365} It increases vaginal weight and vaginal epithelial height (ED50s = 0.48 and 0.39 mg/kg per day, respectively) in an ovariectomized rat model of menopause. Ospemifene also upregulates progesterone receptors in vaginal epithelium and stroma and inhibits estrogen response element-induced transactivation in MCF-7 cells. Formulations containing ospemifene have been used to treat vulvar and vaginal atrophy-induced dyspareunia.
Brand:CaymanSKU:23755 - 50 mgAvailable on backorder
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM) that binds to the estrogen receptors ERα and ERβ (Kis = 380 and 410 nM, respectively).{41365} It increases vaginal weight and vaginal epithelial height (ED50s = 0.48 and 0.39 mg/kg per day, respectively) in an ovariectomized rat model of menopause. Ospemifene also upregulates progesterone receptors in vaginal epithelium and stroma and inhibits estrogen response element-induced transactivation in MCF-7 cells. Formulations containing ospemifene have been used to treat vulvar and vaginal atrophy-induced dyspareunia.
Brand:CaymanSKU:23755 - 500 mgAvailable on backorder
OSS-128167 is an inhibitor of sirtuin 6 (SIRT6; IC50 = 89 μM).{45584} It is selective for SIRT6 over SIRT1 and SIRT2 (IC50s = 1,578 and 751 μM, respectively). OSS-128167 increases acetylation of histone H3 lysine 9 (H3K9) and glucose uptake and decreases TNF-α release in BxPC-3 cells. In vivo, OSS-128167 (100 μg/animal, i.c.v.) prevents decreases in left hemisphere cerebral levels of IL-1β, TNF-α, and IL-6 and neutrophil infiltration induced by bexarotene (Item No. 11571) in a rat model of subarachnoid hemorrhage.{45585}
Brand:CaymanSKU:29052 - 1 mgAvailable on backorder
OSS-128167 is an inhibitor of sirtuin 6 (SIRT6; IC50 = 89 μM).{45584} It is selective for SIRT6 over SIRT1 and SIRT2 (IC50s = 1,578 and 751 μM, respectively). OSS-128167 increases acetylation of histone H3 lysine 9 (H3K9) and glucose uptake and decreases TNF-α release in BxPC-3 cells. In vivo, OSS-128167 (100 μg/animal, i.c.v.) prevents decreases in left hemisphere cerebral levels of IL-1β, TNF-α, and IL-6 and neutrophil infiltration induced by bexarotene (Item No. 11571) in a rat model of subarachnoid hemorrhage.{45585}
Brand:CaymanSKU:29052 - 10 mgAvailable on backorder
OSS-128167 is an inhibitor of sirtuin 6 (SIRT6; IC50 = 89 μM).{45584} It is selective for SIRT6 over SIRT1 and SIRT2 (IC50s = 1,578 and 751 μM, respectively). OSS-128167 increases acetylation of histone H3 lysine 9 (H3K9) and glucose uptake and decreases TNF-α release in BxPC-3 cells. In vivo, OSS-128167 (100 μg/animal, i.c.v.) prevents decreases in left hemisphere cerebral levels of IL-1β, TNF-α, and IL-6 and neutrophil infiltration induced by bexarotene (Item No. 11571) in a rat model of subarachnoid hemorrhage.{45585}
Brand:CaymanSKU:29052 - 25 mgAvailable on backorder
OSS-128167 is an inhibitor of sirtuin 6 (SIRT6; IC50 = 89 μM).{45584} It is selective for SIRT6 over SIRT1 and SIRT2 (IC50s = 1,578 and 751 μM, respectively). OSS-128167 increases acetylation of histone H3 lysine 9 (H3K9) and glucose uptake and decreases TNF-α release in BxPC-3 cells. In vivo, OSS-128167 (100 μg/animal, i.c.v.) prevents decreases in left hemisphere cerebral levels of IL-1β, TNF-α, and IL-6 and neutrophil infiltration induced by bexarotene (Item No. 11571) in a rat model of subarachnoid hemorrhage.{45585}
Brand:CaymanSKU:29052 - 5 mgAvailable on backorder
Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone.{39529} Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget’s disease, and primary hyperparathyroidism.{39529,39530} Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women.{39531} In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics.{39530} It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.{39532}
Brand:CaymanSKU:24723 - 100 µgAvailable on backorder
Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone.{39529} Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget’s disease, and primary hyperparathyroidism.{39529,39530} Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women.{39531} In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics.{39530} It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.{39532}
Brand:CaymanSKU:24723 - 500 µgAvailable on backorder
Osthole is a coumarin that has been found in C. monnieri and has diverse biological activities.{31047,31048,31049} It decreases secretion of hepatitis B surface antigen (HBsAg) from Huh7 cells transfected with hepatitis B virus (HBV) DNA by 70% when used at a concentration of 20 µg/ml.{31047} Osthole induces bone morphogenetic protein 2 (BMP2) production in and differentiation of MG-63 and hFOB osteoblast-like cells.{31048} It induces vasorelaxation in isolated rat blood vessels, ileum, corpus cavernosum, and trachea.{31049} Osthole inhibits migration and invasion of MCF-7, MDA-MB-231, H1299, and A549 cancer cells in vitro and increases survival in an SMMC-7721 hepatocellular carcinoma mouse xenograft model. It also has hepatoprotective effects in mouse models of hepatitis induced by concanavalin A (Item No. 14951) and alcoholic fatty liver disease.
Brand:CaymanSKU:-Available on backorder
Osthole is a coumarin that has been found in C. monnieri and has diverse biological activities.{31047,31048,31049} It decreases secretion of hepatitis B surface antigen (HBsAg) from Huh7 cells transfected with hepatitis B virus (HBV) DNA by 70% when used at a concentration of 20 µg/ml.{31047} Osthole induces bone morphogenetic protein 2 (BMP2) production in and differentiation of MG-63 and hFOB osteoblast-like cells.{31048} It induces vasorelaxation in isolated rat blood vessels, ileum, corpus cavernosum, and trachea.{31049} Osthole inhibits migration and invasion of MCF-7, MDA-MB-231, H1299, and A549 cancer cells in vitro and increases survival in an SMMC-7721 hepatocellular carcinoma mouse xenograft model. It also has hepatoprotective effects in mouse models of hepatitis induced by concanavalin A (Item No. 14951) and alcoholic fatty liver disease.
Brand:CaymanSKU:-Available on backorder
Osthole is a coumarin that has been found in C. monnieri and has diverse biological activities.{31047,31048,31049} It decreases secretion of hepatitis B surface antigen (HBsAg) from Huh7 cells transfected with hepatitis B virus (HBV) DNA by 70% when used at a concentration of 20 µg/ml.{31047} Osthole induces bone morphogenetic protein 2 (BMP2) production in and differentiation of MG-63 and hFOB osteoblast-like cells.{31048} It induces vasorelaxation in isolated rat blood vessels, ileum, corpus cavernosum, and trachea.{31049} Osthole inhibits migration and invasion of MCF-7, MDA-MB-231, H1299, and A549 cancer cells in vitro and increases survival in an SMMC-7721 hepatocellular carcinoma mouse xenograft model. It also has hepatoprotective effects in mouse models of hepatitis induced by concanavalin A (Item No. 14951) and alcoholic fatty liver disease.
Brand:CaymanSKU:-Available on backorder
Osthole is a coumarin that has been found in C. monnieri and has diverse biological activities.{31047,31048,31049} It decreases secretion of hepatitis B surface antigen (HBsAg) from Huh7 cells transfected with hepatitis B virus (HBV) DNA by 70% when used at a concentration of 20 µg/ml.{31047} Osthole induces bone morphogenetic protein 2 (BMP2) production in and differentiation of MG-63 and hFOB osteoblast-like cells.{31048} It induces vasorelaxation in isolated rat blood vessels, ileum, corpus cavernosum, and trachea.{31049} Osthole inhibits migration and invasion of MCF-7, MDA-MB-231, H1299, and A549 cancer cells in vitro and increases survival in an SMMC-7721 hepatocellular carcinoma mouse xenograft model. It also has hepatoprotective effects in mouse models of hepatitis induced by concanavalin A (Item No. 14951) and alcoholic fatty liver disease.
Brand:CaymanSKU:-Available on backorder
Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity.{11047} OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway.{13637,13638,13639} It has an IC50 value of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM.{13638} OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.{13638} It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.{13639} OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.{13637}
Brand:CaymanSKU:10008005 - 10 mgAvailable on backorder
Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity.{11047} OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway.{13637,13638,13639} It has an IC50 value of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM.{13638} OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.{13638} It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.{13639} OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.{13637}
Brand:CaymanSKU:10008005 - 100 mgAvailable on backorder
Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity.{11047} OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway.{13637,13638,13639} It has an IC50 value of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM.{13638} OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.{13638} It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.{13639} OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.{13637}
Brand:CaymanSKU:10008005 - 5 mgAvailable on backorder
Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity.{11047} OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway.{13637,13638,13639} It has an IC50 value of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM.{13638} OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.{13638} It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.{13639} OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.{13637}
Brand:CaymanSKU:10008005 - 50 mgAvailable on backorder
OSW-1 is a saponin that has been found in O. saundersiae and has antiviral and anticancer activities.{53441} It is an inhibitor of oxysterol-binding protein (OSBP) and its paralog OSBP-related protein 4 (ORP4) with Ki values of 16 and 71 nM, respectively, in radioligand binding assays using HEK293T cell lysates.{53442} It induces OSBP translocalization from the cytoplasm to the trans-Golgi network and decreases intracellular levels of OSBP in HEK293 cells.{53442,45822} OSW-1 inhibits replication of a variety of enteroviruses (IC50s = 2.4-9.4 nM), including replication of coxsackievirus B3 (CVB3) in infected HeLa R19 cells in an OSBP-dependent manner when used at a concentration of 3 nM.{53443} It also inhibits replication of hepatitis C virus (HCV) but not mouse hepatitis virus (MHV), a coronavirus.{45895} It protects against CVA9 and echovirus 2 infection in HeLa cells when used at a concentration of 10 nM.{53443} OSW-1 inhibits growth of HeLa and HEK293 cells (GI50s = 0.33 and 0.22 nM, respectively).{53442}
Brand:CaymanSKU:30310 - 1 mgAvailable on backorder
OSW-1 is a saponin that has been found in O. saundersiae and has antiviral and anticancer activities.{53441} It is an inhibitor of oxysterol-binding protein (OSBP) and its paralog OSBP-related protein 4 (ORP4) with Ki values of 16 and 71 nM, respectively, in radioligand binding assays using HEK293T cell lysates.{53442} It induces OSBP translocalization from the cytoplasm to the trans-Golgi network and decreases intracellular levels of OSBP in HEK293 cells.{53442,45822} OSW-1 inhibits replication of a variety of enteroviruses (IC50s = 2.4-9.4 nM), including replication of coxsackievirus B3 (CVB3) in infected HeLa R19 cells in an OSBP-dependent manner when used at a concentration of 3 nM.{53443} It also inhibits replication of hepatitis C virus (HCV) but not mouse hepatitis virus (MHV), a coronavirus.{45895} It protects against CVA9 and echovirus 2 infection in HeLa cells when used at a concentration of 10 nM.{53443} OSW-1 inhibits growth of HeLa and HEK293 cells (GI50s = 0.33 and 0.22 nM, respectively).{53442}
Brand:CaymanSKU:30310 - 5 mgAvailable on backorder
OSW-1 is a saponin that has been found in O. saundersiae and has antiviral and anticancer activities.{53441} It is an inhibitor of oxysterol-binding protein (OSBP) and its paralog OSBP-related protein 4 (ORP4) with Ki values of 16 and 71 nM, respectively, in radioligand binding assays using HEK293T cell lysates.{53442} It induces OSBP translocalization from the cytoplasm to the trans-Golgi network and decreases intracellular levels of OSBP in HEK293 cells.{53442,45822} OSW-1 inhibits replication of a variety of enteroviruses (IC50s = 2.4-9.4 nM), including replication of coxsackievirus B3 (CVB3) in infected HeLa R19 cells in an OSBP-dependent manner when used at a concentration of 3 nM.{53443} It also inhibits replication of hepatitis C virus (HCV) but not mouse hepatitis virus (MHV), a coronavirus.{45895} It protects against CVA9 and echovirus 2 infection in HeLa cells when used at a concentration of 10 nM.{53443} OSW-1 inhibits growth of HeLa and HEK293 cells (GI50s = 0.33 and 0.22 nM, respectively).{53442}
Brand:CaymanSKU:30310 - 500 µgAvailable on backorder
Otilonium is an inhibitor of L-type (IC50 = 2.3 µM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 µM for Cav3.1, Cav3.2, and Cav3.3, respectively).{46774,46775} It is also an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 µM).{46778} Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine (Item No. 11106).{46774} It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM).{46776} Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.{46777}
Brand:CaymanSKU:29907 - 10 mgAvailable on backorder
Otilonium is an inhibitor of L-type (IC50 = 2.3 µM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 µM for Cav3.1, Cav3.2, and Cav3.3, respectively).{46774,46775} It is also an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 µM).{46778} Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine (Item No. 11106).{46774} It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM).{46776} Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.{46777}
Brand:CaymanSKU:29907 - 100 mgAvailable on backorder
Otilonium is an inhibitor of L-type (IC50 = 2.3 µM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 µM for Cav3.1, Cav3.2, and Cav3.3, respectively).{46774,46775} It is also an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 µM).{46778} Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine (Item No. 11106).{46774} It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM).{46776} Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.{46777}
Brand:CaymanSKU:29907 - 250 mgAvailable on backorder
Otilonium is an inhibitor of L-type (IC50 = 2.3 µM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 µM for Cav3.1, Cav3.2, and Cav3.3, respectively).{46774,46775} It is also an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 µM).{46778} Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine (Item No. 11106).{46774} It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM).{46776} Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.{46777}
Brand:CaymanSKU:29907 - 50 mgAvailable on backorder
OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer.{32494,37578} OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM).{37579,37580,32493} In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.{32494}
Brand:CaymanSKU:-Out of stock
OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer.{32494,37578} OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM).{37579,37580,32493} In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.{32494}
Brand:CaymanSKU:-Out of stock
OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer.{32494,37578} OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM).{37579,37580,32493} In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.{32494}
Brand:CaymanSKU:-Out of stock
OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM).{32494} It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells.{32494,32493} OTS964 induces apoptosis of human lung cancer cells in mouse xenografts.{32494}
Brand:CaymanSKU:-Out of stock
OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM).{32494} It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells.{32494,32493} OTS964 induces apoptosis of human lung cancer cells in mouse xenografts.{32494}
Brand:CaymanSKU:-Out of stock
OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM).{32494} It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells.{32494,32493} OTS964 induces apoptosis of human lung cancer cells in mouse xenografts.{32494}
Brand:CaymanSKU:-Out of stock
Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.{27684} MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.{27683,24926,24930} OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).{27685} It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.{27685} It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.{27685} OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.{27685,27686}
Brand:CaymanSKU:-Out of stock
Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.{27684} MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.{27683,24926,24930} OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).{27685} It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.{27685} It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.{27685} OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.{27685,27686}
Brand:CaymanSKU:-Out of stock
Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.{27684} MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.{27683,24926,24930} OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).{27685} It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.{27685} It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.{27685} OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.{27685,27686}
Brand:CaymanSKU:-Out of stock
OTX008 is a small molecule topomimetic of the antiangiogenic peptide anginex and an inhibitor of galectin-1 (Gal-1).{41594} It decreases lactose binding to Gal-1 with Kd values of 290 and 100 μM in the presence and absence of OTX008, respectively, and is cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression. OTX008 inhibits proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay.{41595} OTX008 is angiostatic in a chorioallantoic membrane (CAM) assay, inducing formation of shorter, finer, and less defined vessels than vehicle control in fertilized chicken eggs. In vivo, OTX008 (2.4 and 10 mg/kg) reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis.
Brand:CaymanSKU:23130 - 1 mgAvailable on backorder
OTX008 is a small molecule topomimetic of the antiangiogenic peptide anginex and an inhibitor of galectin-1 (Gal-1).{41594} It decreases lactose binding to Gal-1 with Kd values of 290 and 100 μM in the presence and absence of OTX008, respectively, and is cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression. OTX008 inhibits proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay.{41595} OTX008 is angiostatic in a chorioallantoic membrane (CAM) assay, inducing formation of shorter, finer, and less defined vessels than vehicle control in fertilized chicken eggs. In vivo, OTX008 (2.4 and 10 mg/kg) reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis.
Brand:CaymanSKU:23130 - 10 mgAvailable on backorder
OTX008 is a small molecule topomimetic of the antiangiogenic peptide anginex and an inhibitor of galectin-1 (Gal-1).{41594} It decreases lactose binding to Gal-1 with Kd values of 290 and 100 μM in the presence and absence of OTX008, respectively, and is cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression. OTX008 inhibits proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay.{41595} OTX008 is angiostatic in a chorioallantoic membrane (CAM) assay, inducing formation of shorter, finer, and less defined vessels than vehicle control in fertilized chicken eggs. In vivo, OTX008 (2.4 and 10 mg/kg) reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis.
Brand:CaymanSKU:23130 - 5 mgAvailable on backorder
OTX008 is a small molecule topomimetic of the antiangiogenic peptide anginex and an inhibitor of galectin-1 (Gal-1).{41594} It decreases lactose binding to Gal-1 with Kd values of 290 and 100 μM in the presence and absence of OTX008, respectively, and is cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression. OTX008 inhibits proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay.{41595} OTX008 is angiostatic in a chorioallantoic membrane (CAM) assay, inducing formation of shorter, finer, and less defined vessels than vehicle control in fertilized chicken eggs. In vivo, OTX008 (2.4 and 10 mg/kg) reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis.
Brand:CaymanSKU:23130 - 500 µgAvailable on backorder
The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).{25844} It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.{25844,25845,25843} At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.{25844}
Brand:CaymanSKU:- The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).{25844} It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.{25844,25845,25843} At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.{25844}
Brand:CaymanSKU:- The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).{25844} It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.{25844,25845,25843} At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.{25844}
Brand:CaymanSKU:-