Chemicals
Showing 32401–32550 of 41137 results
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PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
Brand:CaymanSKU:21202 -Out of stock
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
Brand:CaymanSKU:21202 -Out of stock
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
Brand:CaymanSKU:21202 -Out of stock
PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively).{17757} It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.{53121}
Brand:CaymanSKU:27664 - 1 mgAvailable on backorder
PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively).{17757} It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.{53121}
Brand:CaymanSKU:27664 - 10 mgAvailable on backorder
PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively).{17757} It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.{53121}
Brand:CaymanSKU:27664 - 25 mgAvailable on backorder
PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively).{17757} It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.{53121}
Brand:CaymanSKU:27664 - 5 mgAvailable on backorder
The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.{25323} PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}
Brand:CaymanSKU:- The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.{25323} PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}
Brand:CaymanSKU:- The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.{25323} PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}
Brand:CaymanSKU:- The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.{25323} PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}
Brand:CaymanSKU:-
PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM).{39442} It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.{39443}
Brand:CaymanSKU:23974 - 25 mgAvailable on backorder
PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM).{39442} It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.{39443}
Brand:CaymanSKU:23974 - 5 mgAvailable on backorder
PKUMDL-LC-101-D04 is an allosteric activator of glutathione peroxidase 4 (GPX4).{47751} It increases GPX4 activity to 150% of control levels when used at a concentration of 20 μM in a cell-free assay and at 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts. PKUMDL-LC-101-D04 (200 μM) also reduces cholesterol hydroperoxide-induced MEF death.
Brand:CaymanSKU:28966 - 1 mgAvailable on backorder
PKUMDL-LC-101-D04 is an allosteric activator of glutathione peroxidase 4 (GPX4).{47751} It increases GPX4 activity to 150% of control levels when used at a concentration of 20 μM in a cell-free assay and at 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts. PKUMDL-LC-101-D04 (200 μM) also reduces cholesterol hydroperoxide-induced MEF death.
Brand:CaymanSKU:28966 - 5 mgAvailable on backorder
Spliceosomes mediate the processing of pre-mRNA into mature mRNA.{27002,27000} Each spliceosome is a multiunit complex containing several proteins and RNA molecules that work in unison to repeatedly cleave and rejoin segments of mRNA.{27002, 27000} Pladienolide B is a macrocyclic lactone that selectively binds splicing factor 3b and inhibits mRNA splicing.{27003,27004} Through this action, pladienolide B potently blocks the growth of proliferating cells with mean IC50 values of 1.6 nM for six gastric cancer cell lines.{27005,27001} In xenograft tumors generated in mice using human cancer cells, pladienolide B blocks mRNA splicing and induces apoptosis, clearing tumors within two weeks after treatment.{27001}
Brand:CaymanSKU:-Out of stock
Spliceosomes mediate the processing of pre-mRNA into mature mRNA.{27002,27000} Each spliceosome is a multiunit complex containing several proteins and RNA molecules that work in unison to repeatedly cleave and rejoin segments of mRNA.{27002, 27000} Pladienolide B is a macrocyclic lactone that selectively binds splicing factor 3b and inhibits mRNA splicing.{27003,27004} Through this action, pladienolide B potently blocks the growth of proliferating cells with mean IC50 values of 1.6 nM for six gastric cancer cell lines.{27005,27001} In xenograft tumors generated in mice using human cancer cells, pladienolide B blocks mRNA splicing and induces apoptosis, clearing tumors within two weeks after treatment.{27001}
Brand:CaymanSKU:-Out of stock
Plantamajoside is a phenylethanoid that has been found in P. lanceolata and has diverse biological activities, including antioxidative, anticancer, and anti-inflammatory properties.{45282,45283,45284} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in a cell-free assay (IC50 = 11.8 µM). It also inhibits 5-lipoxygenase (5-LO) and 15-LO (IC50s = 0.375 and 96 µM, respectively).{45282,45283} Plantamajoside decreases viability of TE-1 esophageal squamous cell carcinoma (ESCC) cells when used at concentrations ranging from 20 to 320 µg/ml, as well as inhibits LPS-induced epithelial-to-mesenchymal transition (EMT) in Eca-109 and TE-1 cells and decreases phosphorylated NF-κB levels in TE-1 cells.{45284} Plantamajoside (3 mg/ear) inhibits mouse ear edema induced by arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) by 25%.{45282}
Brand:CaymanSKU:27296 - 1 mgAvailable on backorder
Plantamajoside is a phenylethanoid that has been found in P. lanceolata and has diverse biological activities, including antioxidative, anticancer, and anti-inflammatory properties.{45282,45283,45284} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in a cell-free assay (IC50 = 11.8 µM). It also inhibits 5-lipoxygenase (5-LO) and 15-LO (IC50s = 0.375 and 96 µM, respectively).{45282,45283} Plantamajoside decreases viability of TE-1 esophageal squamous cell carcinoma (ESCC) cells when used at concentrations ranging from 20 to 320 µg/ml, as well as inhibits LPS-induced epithelial-to-mesenchymal transition (EMT) in Eca-109 and TE-1 cells and decreases phosphorylated NF-κB levels in TE-1 cells.{45284} Plantamajoside (3 mg/ear) inhibits mouse ear edema induced by arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) by 25%.{45282}
Brand:CaymanSKU:27296 - 10 mgAvailable on backorder
Plantamajoside is a phenylethanoid that has been found in P. lanceolata and has diverse biological activities, including antioxidative, anticancer, and anti-inflammatory properties.{45282,45283,45284} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in a cell-free assay (IC50 = 11.8 µM). It also inhibits 5-lipoxygenase (5-LO) and 15-LO (IC50s = 0.375 and 96 µM, respectively).{45282,45283} Plantamajoside decreases viability of TE-1 esophageal squamous cell carcinoma (ESCC) cells when used at concentrations ranging from 20 to 320 µg/ml, as well as inhibits LPS-induced epithelial-to-mesenchymal transition (EMT) in Eca-109 and TE-1 cells and decreases phosphorylated NF-κB levels in TE-1 cells.{45284} Plantamajoside (3 mg/ear) inhibits mouse ear edema induced by arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) by 25%.{45282}
Brand:CaymanSKU:27296 - 5 mgAvailable on backorder
Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis, which is also the source of platensimycin (Item No. 15507).{25157} Platencin inhibits two key enzymes in bacterial fatty acid synthesis, β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively), unlike platensimycin which only targets FabF.{25157} The IC50 values for platencin against FabF and FabH are 1.95 and 3.91 μg/ml, respectively.{25157} It does not exhibit cross-resistance to antibiotic resistant bacterial strains, including methicillin-resistant S. aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci.{25157} For these reasons, platencin has potential applications in fighting antibiotic resistant bacteria.{25158,25108}
Brand:CaymanSKU:- Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis, which is also the source of platensimycin (Item No. 15507).{25157} Platencin inhibits two key enzymes in bacterial fatty acid synthesis, β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively), unlike platensimycin which only targets FabF.{25157} The IC50 values for platencin against FabF and FabH are 1.95 and 3.91 μg/ml, respectively.{25157} It does not exhibit cross-resistance to antibiotic resistant bacterial strains, including methicillin-resistant S. aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci.{25157} For these reasons, platencin has potential applications in fighting antibiotic resistant bacteria.{25158,25108}
Brand:CaymanSKU:-
Platensimycin (PTM) is an antibiotic produced by S. platensis that inhibits Gram-positve bacteria by selectively inhibiting cellular lipid biosynthesis (IC50 = 0.1 μM).{25106} It targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s = 48 and 160 nM for S. aureus and E. coli enzymes, respectively).{25106} By specifically targeting fatty acid synthesis in bacteria, PTM is thought to be a promising agent for overcoming antibiotic resistance.{25108} PTM is also a selective inhibitor of the mammalian fatty acid synthase and has been shown to reduce liver triglyceride levels and to improve insulin sensitivity in a diabetic mouse model after an oral dose of 30 mg/kg.{25107}
Brand:CaymanSKU:- Platensimycin (PTM) is an antibiotic produced by S. platensis that inhibits Gram-positve bacteria by selectively inhibiting cellular lipid biosynthesis (IC50 = 0.1 μM).{25106} It targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s = 48 and 160 nM for S. aureus and E. coli enzymes, respectively).{25106} By specifically targeting fatty acid synthesis in bacteria, PTM is thought to be a promising agent for overcoming antibiotic resistance.{25108} PTM is also a selective inhibitor of the mammalian fatty acid synthase and has been shown to reduce liver triglyceride levels and to improve insulin sensitivity in a diabetic mouse model after an oral dose of 30 mg/kg.{25107}
Brand:CaymanSKU:-
Platycodin D is a saponin isolated from the root of P. grandiflorum. Root preparations have been used extensively in Chinese herbal medicine for many applications, particularly for upper respiratory disorders and inflammation.{20971} The cellular and physiological actions of purified platycodin D have not been elucidated.
Brand:CaymanSKU:11725 - 1 mgAvailable on backorder
Platycodin D is a saponin isolated from the root of P. grandiflorum. Root preparations have been used extensively in Chinese herbal medicine for many applications, particularly for upper respiratory disorders and inflammation.{20971} The cellular and physiological actions of purified platycodin D have not been elucidated.
Brand:CaymanSKU:11725 - 10 mgAvailable on backorder
Platycodin D is a saponin isolated from the root of P. grandiflorum. Root preparations have been used extensively in Chinese herbal medicine for many applications, particularly for upper respiratory disorders and inflammation.{20971} The cellular and physiological actions of purified platycodin D have not been elucidated.
Brand:CaymanSKU:11725 - 25 mgAvailable on backorder
Platycodin D is a saponin isolated from the root of P. grandiflorum. Root preparations have been used extensively in Chinese herbal medicine for many applications, particularly for upper respiratory disorders and inflammation.{20971} The cellular and physiological actions of purified platycodin D have not been elucidated.
Brand:CaymanSKU:11725 - 5 mgAvailable on backorder
Pleconaril is an antipicornaviral agent.{52019, 52020} It inhibits Picornaviridae viral replication by binding to a hydrophobic pocket in the major VP1 capsid protein, which prevents uncoating of the viral RNA genome. Pleconaril inhibits replication of the rhinoviruses HRV-A2 and HRV-B14 in HeLa Rh cells (EC50s = 0.1 and 0.3 μM, respectively) and is not cytotoxic to HeLa Rh cells with a 50% cytotoxic concentration (CC50) of greater than 131 μM.{52020} It also inhibits replication of enterovirus 71 (EV71) in human rhabdomyosarcoma (RD) cells (EC50 = 15 μM) and is not cytotoxic to RD cells (CC50 = >131 μM). Pleconaril (80 mg/kg per day) increases survival of EV71-infected mouse pups from 20 to 80%.{52021}
Brand:CaymanSKU:28461 - 10 mgAvailable on backorder
Pleconaril is an antipicornaviral agent.{52019, 52020} It inhibits Picornaviridae viral replication by binding to a hydrophobic pocket in the major VP1 capsid protein, which prevents uncoating of the viral RNA genome. Pleconaril inhibits replication of the rhinoviruses HRV-A2 and HRV-B14 in HeLa Rh cells (EC50s = 0.1 and 0.3 μM, respectively) and is not cytotoxic to HeLa Rh cells with a 50% cytotoxic concentration (CC50) of greater than 131 μM.{52020} It also inhibits replication of enterovirus 71 (EV71) in human rhabdomyosarcoma (RD) cells (EC50 = 15 μM) and is not cytotoxic to RD cells (CC50 = >131 μM). Pleconaril (80 mg/kg per day) increases survival of EV71-infected mouse pups from 20 to 80%.{52021}
Brand:CaymanSKU:28461 - 100 mgAvailable on backorder
Pleconaril is an antipicornaviral agent.{52019, 52020} It inhibits Picornaviridae viral replication by binding to a hydrophobic pocket in the major VP1 capsid protein, which prevents uncoating of the viral RNA genome. Pleconaril inhibits replication of the rhinoviruses HRV-A2 and HRV-B14 in HeLa Rh cells (EC50s = 0.1 and 0.3 μM, respectively) and is not cytotoxic to HeLa Rh cells with a 50% cytotoxic concentration (CC50) of greater than 131 μM.{52020} It also inhibits replication of enterovirus 71 (EV71) in human rhabdomyosarcoma (RD) cells (EC50 = 15 μM) and is not cytotoxic to RD cells (CC50 = >131 μM). Pleconaril (80 mg/kg per day) increases survival of EV71-infected mouse pups from 20 to 80%.{52021}
Brand:CaymanSKU:28461 - 25 mgAvailable on backorder
Pleconaril is an antipicornaviral agent.{52019, 52020} It inhibits Picornaviridae viral replication by binding to a hydrophobic pocket in the major VP1 capsid protein, which prevents uncoating of the viral RNA genome. Pleconaril inhibits replication of the rhinoviruses HRV-A2 and HRV-B14 in HeLa Rh cells (EC50s = 0.1 and 0.3 μM, respectively) and is not cytotoxic to HeLa Rh cells with a 50% cytotoxic concentration (CC50) of greater than 131 μM.{52020} It also inhibits replication of enterovirus 71 (EV71) in human rhabdomyosarcoma (RD) cells (EC50 = 15 μM) and is not cytotoxic to RD cells (CC50 = >131 μM). Pleconaril (80 mg/kg per day) increases survival of EV71-infected mouse pups from 20 to 80%.{52021}
Brand:CaymanSKU:28461 - 50 mgAvailable on backorder
The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:10011332 - 1 mgAvailable on backorder
The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:10011332 - 10 mgAvailable on backorder
The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:10011332 - 5 mgAvailable on backorder
The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:10011332 - 50 mgAvailable on backorder
Plerixafor-d4 is intended for use as an internal standard for the quantification of plerixafor (Item No. 10011332) by GC- or LC-MS. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:26490 - 1 mgAvailable on backorder
Plerixafor-d4 is intended for use as an internal standard for the quantification of plerixafor (Item No. 10011332) by GC- or LC-MS. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC50 values ranging from 0.02 to 0.13 µg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells.{42569} It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml).{16446} It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF.{15446} Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system.{16445,16447} Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.{15450}
Brand:CaymanSKU:26490 - 500 µgAvailable on backorder
Pleuromutilin is an antibiotic derived from the fungus Clitopilus that inhibits bacterial protein synthesis by binding to bacterial ribosomes in the peptidyl transferase component of the 50S subunit and inhibiting peptide bond formation.{31436,31437}
Brand:CaymanSKU:-Available on backorder
Pleuromutilin is an antibiotic derived from the fungus Clitopilus that inhibits bacterial protein synthesis by binding to bacterial ribosomes in the peptidyl transferase component of the 50S subunit and inhibiting peptide bond formation.{31436,31437}
Brand:CaymanSKU:-Available on backorder
Pleuromutilin is an antibiotic derived from the fungus Clitopilus that inhibits bacterial protein synthesis by binding to bacterial ribosomes in the peptidyl transferase component of the 50S subunit and inhibiting peptide bond formation.{31436,31437}
Brand:CaymanSKU:-Available on backorder
Pleuromutilin is an antibiotic derived from the fungus Clitopilus that inhibits bacterial protein synthesis by binding to bacterial ribosomes in the peptidyl transferase component of the 50S subunit and inhibiting peptide bond formation.{31436,31437}
Brand:CaymanSKU:-Available on backorder
Plinabulin is a diketopiperazine that induces complete tubulin depolymerization in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 2 μM.{39590} It induces HUVEC monolayer permeability, a marker of vascular collapse, in vitro. Plinabulin is cytotoxic against a panel of cancer cell lines, including the multidrug-resistant MES-SA/Dx5 and HL-60/MX2 cell lines (IC50s = 4.3-18 nM). It induces cell death in patient-derived multiple myeloma cells without affecting viability of peripheral blood mononuclear cells (PBMCs) via inhibition of tubule formation and cell migration as well as induction of mitotic arrest and apoptosis in a JNK-dependent manner.{39591} Plinabulin (7.5 mg/kg) reduces tumor size and increases survival in a MM.1S multiple myeloma mouse xenograft model. Formulations containing plinabulin are under clinical investigation for the treatment of solid tumors and lymphomas.
Brand:CaymanSKU:24190 - 10 mgAvailable on backorder
Plinabulin is a diketopiperazine that induces complete tubulin depolymerization in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 2 μM.{39590} It induces HUVEC monolayer permeability, a marker of vascular collapse, in vitro. Plinabulin is cytotoxic against a panel of cancer cell lines, including the multidrug-resistant MES-SA/Dx5 and HL-60/MX2 cell lines (IC50s = 4.3-18 nM). It induces cell death in patient-derived multiple myeloma cells without affecting viability of peripheral blood mononuclear cells (PBMCs) via inhibition of tubule formation and cell migration as well as induction of mitotic arrest and apoptosis in a JNK-dependent manner.{39591} Plinabulin (7.5 mg/kg) reduces tumor size and increases survival in a MM.1S multiple myeloma mouse xenograft model. Formulations containing plinabulin are under clinical investigation for the treatment of solid tumors and lymphomas.
Brand:CaymanSKU:24190 - 25 mgAvailable on backorder
Plinabulin is a diketopiperazine that induces complete tubulin depolymerization in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 2 μM.{39590} It induces HUVEC monolayer permeability, a marker of vascular collapse, in vitro. Plinabulin is cytotoxic against a panel of cancer cell lines, including the multidrug-resistant MES-SA/Dx5 and HL-60/MX2 cell lines (IC50s = 4.3-18 nM). It induces cell death in patient-derived multiple myeloma cells without affecting viability of peripheral blood mononuclear cells (PBMCs) via inhibition of tubule formation and cell migration as well as induction of mitotic arrest and apoptosis in a JNK-dependent manner.{39591} Plinabulin (7.5 mg/kg) reduces tumor size and increases survival in a MM.1S multiple myeloma mouse xenograft model. Formulations containing plinabulin are under clinical investigation for the treatment of solid tumors and lymphomas.
Brand:CaymanSKU:24190 - 5 mgAvailable on backorder
Plinabulin is a diketopiperazine that induces complete tubulin depolymerization in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 2 μM.{39590} It induces HUVEC monolayer permeability, a marker of vascular collapse, in vitro. Plinabulin is cytotoxic against a panel of cancer cell lines, including the multidrug-resistant MES-SA/Dx5 and HL-60/MX2 cell lines (IC50s = 4.3-18 nM). It induces cell death in patient-derived multiple myeloma cells without affecting viability of peripheral blood mononuclear cells (PBMCs) via inhibition of tubule formation and cell migration as well as induction of mitotic arrest and apoptosis in a JNK-dependent manner.{39591} Plinabulin (7.5 mg/kg) reduces tumor size and increases survival in a MM.1S multiple myeloma mouse xenograft model. Formulations containing plinabulin are under clinical investigation for the treatment of solid tumors and lymphomas.
Brand:CaymanSKU:24190 - 50 mgAvailable on backorder
Plumbagin is a natural 1,4-naphthoquinone first isolated from plants of the genus Plumbago. It has diverse effects in cells and animals. Plumbagin causes the generation of reactive oxygen species and induces apoptosis in cancer cells.{28824,25057} It activates signaling through Nrf2 and the antioxidant response element, inducing the expression of Nrf2 target genes, including NQO1 and heme oxygenase-1 in cultured neuronal cells.{28824} Plumbagin also inhibits NADPH oxidase 4 in a time- and dose-dependent manner.{28825} It can be protective against peroxide stress or deprivation of glucose or oxygen.{28824}
Brand:CaymanSKU:- Plumbagin is a natural 1,4-naphthoquinone first isolated from plants of the genus Plumbago. It has diverse effects in cells and animals. Plumbagin causes the generation of reactive oxygen species and induces apoptosis in cancer cells.{28824,25057} It activates signaling through Nrf2 and the antioxidant response element, inducing the expression of Nrf2 target genes, including NQO1 and heme oxygenase-1 in cultured neuronal cells.{28824} Plumbagin also inhibits NADPH oxidase 4 in a time- and dose-dependent manner.{28825} It can be protective against peroxide stress or deprivation of glucose or oxygen.{28824}
Brand:CaymanSKU:- Plumbagin is a natural 1,4-naphthoquinone first isolated from plants of the genus Plumbago. It has diverse effects in cells and animals. Plumbagin causes the generation of reactive oxygen species and induces apoptosis in cancer cells.{28824,25057} It activates signaling through Nrf2 and the antioxidant response element, inducing the expression of Nrf2 target genes, including NQO1 and heme oxygenase-1 in cultured neuronal cells.{28824} Plumbagin also inhibits NADPH oxidase 4 in a time- and dose-dependent manner.{28825} It can be protective against peroxide stress or deprivation of glucose or oxygen.{28824}
Brand:CaymanSKU:-
PluriSln 1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-CoA desaturase, a key enzyme for lipid metabolism that is expressed in human pluripotent stem cells (hPSCs).{26485} PluriSln 1 can selectively induce ER stress, attenuate protein synthesis, and induce apoptosis in hPSCs (EC50 = 2 µM) while sparing progenitor and differentiated cells.{26485} Because PluriSln 1 can selectively eliminate undifferentiated hPSCs, it was developed as a strategy to prevent tumorigenic risk from residual undifferentiated cells used during stem cell therapy. In immunocompromised mice, PluriSln 1 has been shown to effectively prevent teratoma formation from undifferentiated hPSCs.{26485}
Brand:CaymanSKU:- PluriSln 1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-CoA desaturase, a key enzyme for lipid metabolism that is expressed in human pluripotent stem cells (hPSCs).{26485} PluriSln 1 can selectively induce ER stress, attenuate protein synthesis, and induce apoptosis in hPSCs (EC50 = 2 µM) while sparing progenitor and differentiated cells.{26485} Because PluriSln 1 can selectively eliminate undifferentiated hPSCs, it was developed as a strategy to prevent tumorigenic risk from residual undifferentiated cells used during stem cell therapy. In immunocompromised mice, PluriSln 1 has been shown to effectively prevent teratoma formation from undifferentiated hPSCs.{26485}
Brand:CaymanSKU:- PluriSln 1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-CoA desaturase, a key enzyme for lipid metabolism that is expressed in human pluripotent stem cells (hPSCs).{26485} PluriSln 1 can selectively induce ER stress, attenuate protein synthesis, and induce apoptosis in hPSCs (EC50 = 2 µM) while sparing progenitor and differentiated cells.{26485} Because PluriSln 1 can selectively eliminate undifferentiated hPSCs, it was developed as a strategy to prevent tumorigenic risk from residual undifferentiated cells used during stem cell therapy. In immunocompromised mice, PluriSln 1 has been shown to effectively prevent teratoma formation from undifferentiated hPSCs.{26485}
Brand:CaymanSKU:- PluriSln 1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-CoA desaturase, a key enzyme for lipid metabolism that is expressed in human pluripotent stem cells (hPSCs).{26485} PluriSln 1 can selectively induce ER stress, attenuate protein synthesis, and induce apoptosis in hPSCs (EC50 = 2 µM) while sparing progenitor and differentiated cells.{26485} Because PluriSln 1 can selectively eliminate undifferentiated hPSCs, it was developed as a strategy to prevent tumorigenic risk from residual undifferentiated cells used during stem cell therapy. In immunocompromised mice, PluriSln 1 has been shown to effectively prevent teratoma formation from undifferentiated hPSCs.{26485}
Brand:CaymanSKU:-
Pluviatolide is a lignan that has been found in B. chinense and has diverse biological activities, including antioxidant, enzyme inhibitory, and antispasmodic properties.{45352,45671,45672} It scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in cell-free assays (IC50s = 23.2 and 88.5 µM, respectively).{45352} Pluviatolide inhibits matrix metalloproteinase-7 (MMP-7) with an IC50 value of 260 µM.{45671} It decreases contractions induced by acetylcholine (Item No. 23829) in isolated guinea pig ileum when used at concentrations of 30 and 100 µM.{45672}
Brand:CaymanSKU:29582 - 1 mgAvailable on backorder
Pluviatolide is a lignan that has been found in B. chinense and has diverse biological activities, including antioxidant, enzyme inhibitory, and antispasmodic properties.{45352,45671,45672} It scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in cell-free assays (IC50s = 23.2 and 88.5 µM, respectively).{45352} Pluviatolide inhibits matrix metalloproteinase-7 (MMP-7) with an IC50 value of 260 µM.{45671} It decreases contractions induced by acetylcholine (Item No. 23829) in isolated guinea pig ileum when used at concentrations of 30 and 100 µM.{45672}
Brand:CaymanSKU:29582 - 5 mgAvailable on backorder
PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively).{27947} It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells.{27947} PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.{18549,18645,27944,27852}
Brand:CaymanSKU:10618 - 10 mgAvailable on backorder
PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively).{27947} It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells.{27947} PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.{18549,18645,27944,27852}
Brand:CaymanSKU:10618 - 25 mgAvailable on backorder
PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively).{27947} It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells.{27947} PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.{18549,18645,27944,27852}
Brand:CaymanSKU:10618 - 5 mgAvailable on backorder
PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively).{27947} It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells.{27947} PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.{18549,18645,27944,27852}
Brand:CaymanSKU:10618 - 50 mgAvailable on backorder
The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).{24814} It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.{24814} PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.{24813,24814,24812}
Brand:CaymanSKU:- The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).{24814} It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.{24814} PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.{24813,24814,24812}
Brand:CaymanSKU:- The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).{24814} It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.{24814} PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.{24813,24814,24812}
Brand:CaymanSKU:- The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).{24814} It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.{24814} PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.{24813,24814,24812}
Brand:CaymanSKU:-
PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.{61018} It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.{61019}
Brand:CaymanSKU:30742 - 1 mgAvailable on backorder
PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.{61018} It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.{61019}
Brand:CaymanSKU:30742 - 5 mgAvailable on backorder
PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.{61018} It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.{61019}
Brand:CaymanSKU:30742 - 500 µgAvailable on backorder
PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (KDR; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}
Brand:CaymanSKU:28927 - 1 mgAvailable on backorder
PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (KDR; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}
Brand:CaymanSKU:28927 - 10 mgAvailable on backorder
PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (KDR; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}
Brand:CaymanSKU:28927 - 25 mgAvailable on backorder
PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (KDR; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}
Brand:CaymanSKU:28927 - 5 mgAvailable on backorder
PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively).{37558} It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
Brand:CaymanSKU:-Available on backorder
PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively).{37558} It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
Brand:CaymanSKU:-Available on backorder
PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively).{37558} It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
Brand:CaymanSKU:-Available on backorder
PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively).{37558} It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
Brand:CaymanSKU:-Available on backorder
PLX7904 is a RAF inhibitor (IC50s = 2.4, 140, and 91 nM for mutant B-RAFV600E, wild-type B-RAF, and C-RAF, respectively).{38489} It inhibits phosphorylation of ERK in A375 and COLO 829 cells (IC50s = 16 and 18 nM, respectively). Unlike PLX4032 (Item No. 10618), BAY 43-9006 (Item No. 10009644), and dabrafenib (Item No. 16989), PLX7904 does not induce paradoxical pERK activation and proliferation of cancer cell lines (EC50s = >200 μM). PLX7904 (25 mg/kg twice per day) inhibits tumor growth in a mouse COLO 205 colon cancer xenograft model.
Brand:CaymanSKU:20710 -Available on backorder
PLX7904 is a RAF inhibitor (IC50s = 2.4, 140, and 91 nM for mutant B-RAFV600E, wild-type B-RAF, and C-RAF, respectively).{38489} It inhibits phosphorylation of ERK in A375 and COLO 829 cells (IC50s = 16 and 18 nM, respectively). Unlike PLX4032 (Item No. 10618), BAY 43-9006 (Item No. 10009644), and dabrafenib (Item No. 16989), PLX7904 does not induce paradoxical pERK activation and proliferation of cancer cell lines (EC50s = >200 μM). PLX7904 (25 mg/kg twice per day) inhibits tumor growth in a mouse COLO 205 colon cancer xenograft model.
Brand:CaymanSKU:20710 -Available on backorder
PLX7904 is a RAF inhibitor (IC50s = 2.4, 140, and 91 nM for mutant B-RAFV600E, wild-type B-RAF, and C-RAF, respectively).{38489} It inhibits phosphorylation of ERK in A375 and COLO 829 cells (IC50s = 16 and 18 nM, respectively). Unlike PLX4032 (Item No. 10618), BAY 43-9006 (Item No. 10009644), and dabrafenib (Item No. 16989), PLX7904 does not induce paradoxical pERK activation and proliferation of cancer cell lines (EC50s = >200 μM). PLX7904 (25 mg/kg twice per day) inhibits tumor growth in a mouse COLO 205 colon cancer xenograft model.
Brand:CaymanSKU:20710 -Available on backorder
PLX7904 is a RAF inhibitor (IC50s = 2.4, 140, and 91 nM for mutant B-RAFV600E, wild-type B-RAF, and C-RAF, respectively).{38489} It inhibits phosphorylation of ERK in A375 and COLO 829 cells (IC50s = 16 and 18 nM, respectively). Unlike PLX4032 (Item No. 10618), BAY 43-9006 (Item No. 10009644), and dabrafenib (Item No. 16989), PLX7904 does not induce paradoxical pERK activation and proliferation of cancer cell lines (EC50s = >200 μM). PLX7904 (25 mg/kg twice per day) inhibits tumor growth in a mouse COLO 205 colon cancer xenograft model.
Brand:CaymanSKU:20710 -Available on backorder
PMK ethyl glycidate (Item No. 21990) is an analytical reference standard that is categorized as a precursor in the synthesis of methylenedioxy phenethylamines and amphetamines, including 3,4-MDMA (Item Nos. 13971 | ISO60190). This product is intended for research and forensic applications.
Brand:CaymanSKU:21990 -Out of stock