Chemicals
Showing 18301–18450 of 41137 results
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Econazole (nitrate) is an azole-based antifungal compound that acts by inhibiting the 14α-demethylation of lanosterol (Item No. 19521), which consequently leads to the inhibition of ergosterol (Item No. 19850) synthesis in fungal cell membranes.{25584} It demonstrates broad-spectrum activity against dermatophytes, Candida species, other pathogenic yeasts, and some Gram-positive bacteria.{25584}
Brand:CaymanSKU:20223 -Available on backorder
Econazole (nitrate) is an azole-based antifungal compound that acts by inhibiting the 14α-demethylation of lanosterol (Item No. 19521), which consequently leads to the inhibition of ergosterol (Item No. 19850) synthesis in fungal cell membranes.{25584} It demonstrates broad-spectrum activity against dermatophytes, Candida species, other pathogenic yeasts, and some Gram-positive bacteria.{25584}
Brand:CaymanSKU:20223 -Available on backorder
Ectoine is a microbial metabolite that has been found in extremophilic bacteria and has photoprotectant and anti-inflammatory activities.{54497,54498} It is biosynthesized in bacteria that grow in extreme conditions, such as high temperatures, intensive sun irradiation, and drought, to protect macromolecules against environmental stressors. Ectoine (1 mM) reduces UVA-induced AP-2 activation, ICAM1 expression, and second messenger release in isolated human keratinocytes.{54497} In vivo, ectoine (100 mg/kg) reduces intestinal crypt damage, edema, and leukocyte infiltration in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{54498}
Brand:CaymanSKU:31167 - 10 gAvailable on backorder
Ectoine is a microbial metabolite that has been found in extremophilic bacteria and has photoprotectant and anti-inflammatory activities.{54497,54498} It is biosynthesized in bacteria that grow in extreme conditions, such as high temperatures, intensive sun irradiation, and drought, to protect macromolecules against environmental stressors. Ectoine (1 mM) reduces UVA-induced AP-2 activation, ICAM1 expression, and second messenger release in isolated human keratinocytes.{54497} In vivo, ectoine (100 mg/kg) reduces intestinal crypt damage, edema, and leukocyte infiltration in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{54498}
Brand:CaymanSKU:31167 - 25 gAvailable on backorder
Ectoine is a microbial metabolite that has been found in extremophilic bacteria and has photoprotectant and anti-inflammatory activities.{54497,54498} It is biosynthesized in bacteria that grow in extreme conditions, such as high temperatures, intensive sun irradiation, and drought, to protect macromolecules against environmental stressors. Ectoine (1 mM) reduces UVA-induced AP-2 activation, ICAM1 expression, and second messenger release in isolated human keratinocytes.{54497} In vivo, ectoine (100 mg/kg) reduces intestinal crypt damage, edema, and leukocyte infiltration in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{54498}
Brand:CaymanSKU:31167 - 5 gAvailable on backorder
Ectoine is a microbial metabolite that has been found in extremophilic bacteria and has photoprotectant and anti-inflammatory activities.{54497,54498} It is biosynthesized in bacteria that grow in extreme conditions, such as high temperatures, intensive sun irradiation, and drought, to protect macromolecules against environmental stressors. Ectoine (1 mM) reduces UVA-induced AP-2 activation, ICAM1 expression, and second messenger release in isolated human keratinocytes.{54497} In vivo, ectoine (100 mg/kg) reduces intestinal crypt damage, edema, and leukocyte infiltration in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{54498}
Brand:CaymanSKU:31167 - 50 gAvailable on backorder
![A PPARγ agonist; activates PPARγ in a reporter assay using CV-1 cells expressing murine PPARγ2 from 0.1-1 μM; increases [3H]2-deoxyglucose transport in the presence and absence of insulin and increases glycogen synthesis in the presence of insulin in soleus muscle strips isolated from obese rats at 1](https://interpriseusa.com/wp-content/uploads/2021/06/19117.png)
Edaglitazone is an agonist of peroxisome proliferator-activated receptor γ (PPARγ).{47216} It activates PPARγ in a reporter assay using CV-1 cells expressing murine PPARγ2 when used at concentrations ranging from 0.1 to 1 μM. Edaglitazone (1, 5, and 25 μM) increases [3H]2-deoxyglucose transport in the presence and absence of insulin and increases glycogen synthesis in the presence of insulin in soleus muscle strips isolated from obese rats.
Brand:CaymanSKU:-Available on backorder
Edaglitazone is an agonist of peroxisome proliferator-activated receptor γ (PPARγ).{47216} It activates PPARγ in a reporter assay using CV-1 cells expressing murine PPARγ2 when used at concentrations ranging from 0.1 to 1 μM. Edaglitazone (1, 5, and 25 μM) increases [3H]2-deoxyglucose transport in the presence and absence of insulin and increases glycogen synthesis in the presence of insulin in soleus muscle strips isolated from obese rats.
Brand:CaymanSKU:-Available on backorder
Edaglitazone is an agonist of peroxisome proliferator-activated receptor γ (PPARγ).{47216} It activates PPARγ in a reporter assay using CV-1 cells expressing murine PPARγ2 when used at concentrations ranging from 0.1 to 1 μM. Edaglitazone (1, 5, and 25 μM) increases [3H]2-deoxyglucose transport in the presence and absence of insulin and increases glycogen synthesis in the presence of insulin in soleus muscle strips isolated from obese rats.
Brand:CaymanSKU:-Available on backorder
EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).{38517} It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM).{38518} EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.
Brand:CaymanSKU:23328 - 1 mgAvailable on backorder
EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).{38517} It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM).{38518} EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.
Brand:CaymanSKU:23328 - 10 mgAvailable on backorder
EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).{38517} It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM).{38518} EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.
Brand:CaymanSKU:23328 - 25 mgAvailable on backorder
EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).{38517} It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM).{38518} EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.
Brand:CaymanSKU:23328 - 5 mgAvailable on backorder
Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).{41299} It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Brand:CaymanSKU:24030 - 1 mgAvailable on backorder
Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).{41299} It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Brand:CaymanSKU:24030 - 5 mgAvailable on backorder
Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).{41299} It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Brand:CaymanSKU:24030 - 500 µgAvailable on backorder
Edoxaban-d6 is intended for use as an internal standard for the quantification of edoxaban (Item No. 24030) by GC- or LC-MS. Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).{41299} It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Brand:CaymanSKU:25760 - 1 mgAvailable on backorder
Edoxaban-d6 is intended for use as an internal standard for the quantification of edoxaban (Item No. 24030) by GC- or LC-MS. Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).{41299} It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Brand:CaymanSKU:25760 - 500 µgAvailable on backorder
Edrophonium (chloride) is an acetylcholinesterase (AChE) inhibitor that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site.{19397} It has been shown to inhibit AChE activity in human red blood cells, purified calf forebrain, and purified octopus brain with Ki values of 0.2, 0.2, and 0.4 µM, respectively.{25818} Edrophonium is often used as part of a battery of pharmacological tests to confirm a diagnosis of the autoimmune neuromuscular junction disorder, myasthenia gravis.{25819}
Brand:CaymanSKU:- Edrophonium (chloride) is an acetylcholinesterase (AChE) inhibitor that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site.{19397} It has been shown to inhibit AChE activity in human red blood cells, purified calf forebrain, and purified octopus brain with Ki values of 0.2, 0.2, and 0.4 µM, respectively.{25818} Edrophonium is often used as part of a battery of pharmacological tests to confirm a diagnosis of the autoimmune neuromuscular junction disorder, myasthenia gravis.{25819}
Brand:CaymanSKU:- Edrophonium (chloride) is an acetylcholinesterase (AChE) inhibitor that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site.{19397} It has been shown to inhibit AChE activity in human red blood cells, purified calf forebrain, and purified octopus brain with Ki values of 0.2, 0.2, and 0.4 µM, respectively.{25818} Edrophonium is often used as part of a battery of pharmacological tests to confirm a diagnosis of the autoimmune neuromuscular junction disorder, myasthenia gravis.{25819}
Brand:CaymanSKU:- Edrophonium (chloride) is an acetylcholinesterase (AChE) inhibitor that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site.{19397} It has been shown to inhibit AChE activity in human red blood cells, purified calf forebrain, and purified octopus brain with Ki values of 0.2, 0.2, and 0.4 µM, respectively.{25818} Edrophonium is often used as part of a battery of pharmacological tests to confirm a diagnosis of the autoimmune neuromuscular junction disorder, myasthenia gravis.{25819}
Brand:CaymanSKU:-
EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2; IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate).{33981} It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on the binding of S-adenosylmethionine-cofactor-competitive inhibitor EI1 (Item No. 19146) to the EZH2 catalytic subunit, indicating EED226 is an allosteric modulator of PRC2 function. EED226 decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner. It also reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo.
Brand:CaymanSKU:22031 -Out of stock
EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2; IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate).{33981} It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on the binding of S-adenosylmethionine-cofactor-competitive inhibitor EI1 (Item No. 19146) to the EZH2 catalytic subunit, indicating EED226 is an allosteric modulator of PRC2 function. EED226 decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner. It also reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo.
Brand:CaymanSKU:22031 -Out of stock
EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2; IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate).{33981} It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on the binding of S-adenosylmethionine-cofactor-competitive inhibitor EI1 (Item No. 19146) to the EZH2 catalytic subunit, indicating EED226 is an allosteric modulator of PRC2 function. EED226 decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner. It also reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo.
Brand:CaymanSKU:22031 -Out of stock
EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2; IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate).{33981} It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on the binding of S-adenosylmethionine-cofactor-competitive inhibitor EI1 (Item No. 19146) to the EZH2 catalytic subunit, indicating EED226 is an allosteric modulator of PRC2 function. EED226 decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner. It also reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo.
Brand:CaymanSKU:22031 -Out of stock
Terminally misfolded proteins, recognized by chaperones on the endoplasmic reticulum (ER), are transported to depots for ubiquitination and proteasomal degradation by the ER-associated protein degradation (ERAD) pathway. Eeyarestatin 1 is an inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM.{15691} It associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3.{27313,27314} Eeyarestatin 1, at 4 µM, interferes with both retrograde and anterograde trafficking of proteins, including certain toxins, and potentially, viruses.{27315}
Brand:CaymanSKU:10012609 - 10 mgAvailable on backorder
Terminally misfolded proteins, recognized by chaperones on the endoplasmic reticulum (ER), are transported to depots for ubiquitination and proteasomal degradation by the ER-associated protein degradation (ERAD) pathway. Eeyarestatin 1 is an inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM.{15691} It associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3.{27313,27314} Eeyarestatin 1, at 4 µM, interferes with both retrograde and anterograde trafficking of proteins, including certain toxins, and potentially, viruses.{27315}
Brand:CaymanSKU:10012609 - 25 mgAvailable on backorder
Terminally misfolded proteins, recognized by chaperones on the endoplasmic reticulum (ER), are transported to depots for ubiquitination and proteasomal degradation by the ER-associated protein degradation (ERAD) pathway. Eeyarestatin 1 is an inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM.{15691} It associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3.{27313,27314} Eeyarestatin 1, at 4 µM, interferes with both retrograde and anterograde trafficking of proteins, including certain toxins, and potentially, viruses.{27315}
Brand:CaymanSKU:10012609 - 5 mgAvailable on backorder
Efaproxiral is an allosteric hemoglobin (Hb) modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue.{51161} In isolated human whole blood, efaproxiral (1.75 mM) increases the partial pressure of oxygen at which Hb is 50% saturated (p50) from 26.75 to 38.63 mm Hg and decreases the percent oxyhemoglobin (Hb-O2) saturation from 48 to 33.8% at a partial oxygen pressure (pO2) of 26 mm Hg. Efaproxiral (150 mg/kg) increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model.{51162} Efaproxiral (100 μM) enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions and increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model when administered at a dose of 100 mg/kg.{51163} It also increases the running capacity of normal mice and mice with left coronary artery (LCA) ligation-induced myocardial infarction (MI) when administered at a dose of 150 mg/kg.{51164}
Brand:CaymanSKU:28294 - 1 gAvailable on backorder
Efaproxiral is an allosteric hemoglobin (Hb) modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue.{51161} In isolated human whole blood, efaproxiral (1.75 mM) increases the partial pressure of oxygen at which Hb is 50% saturated (p50) from 26.75 to 38.63 mm Hg and decreases the percent oxyhemoglobin (Hb-O2) saturation from 48 to 33.8% at a partial oxygen pressure (pO2) of 26 mm Hg. Efaproxiral (150 mg/kg) increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model.{51162} Efaproxiral (100 μM) enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions and increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model when administered at a dose of 100 mg/kg.{51163} It also increases the running capacity of normal mice and mice with left coronary artery (LCA) ligation-induced myocardial infarction (MI) when administered at a dose of 150 mg/kg.{51164}
Brand:CaymanSKU:28294 - 100 mgAvailable on backorder
Efaproxiral is an allosteric hemoglobin (Hb) modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue.{51161} In isolated human whole blood, efaproxiral (1.75 mM) increases the partial pressure of oxygen at which Hb is 50% saturated (p50) from 26.75 to 38.63 mm Hg and decreases the percent oxyhemoglobin (Hb-O2) saturation from 48 to 33.8% at a partial oxygen pressure (pO2) of 26 mm Hg. Efaproxiral (150 mg/kg) increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model.{51162} Efaproxiral (100 μM) enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions and increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model when administered at a dose of 100 mg/kg.{51163} It also increases the running capacity of normal mice and mice with left coronary artery (LCA) ligation-induced myocardial infarction (MI) when administered at a dose of 150 mg/kg.{51164}
Brand:CaymanSKU:28294 - 250 mgAvailable on backorder
Efaproxiral is an allosteric hemoglobin (Hb) modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue.{51161} In isolated human whole blood, efaproxiral (1.75 mM) increases the partial pressure of oxygen at which Hb is 50% saturated (p50) from 26.75 to 38.63 mm Hg and decreases the percent oxyhemoglobin (Hb-O2) saturation from 48 to 33.8% at a partial oxygen pressure (pO2) of 26 mm Hg. Efaproxiral (150 mg/kg) increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model.{51162} Efaproxiral (100 μM) enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions and increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model when administered at a dose of 100 mg/kg.{51163} It also increases the running capacity of normal mice and mice with left coronary artery (LCA) ligation-induced myocardial infarction (MI) when administered at a dose of 150 mg/kg.{51164}
Brand:CaymanSKU:28294 - 500 mgAvailable on backorder
Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}
Brand:CaymanSKU:29008 - 10 mgAvailable on backorder
Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}
Brand:CaymanSKU:29008 - 25 mgAvailable on backorder
Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}
Brand:CaymanSKU:29008 - 50 mgAvailable on backorder
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).{42187} It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.{22819} In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.{42188} Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.{22821,22820}
Brand:CaymanSKU:- Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).{42187} It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.{22819} In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.{42188} Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.{22821,22820}
Brand:CaymanSKU:- Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).{42187} It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.{22819} In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.{42188} Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.{22821,22820}
Brand:CaymanSKU:- Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).{42187} It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.{22819} In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.{42188} Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.{22821,22820}
Brand:CaymanSKU:-
Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon.{41490} It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane.{41491} It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
Brand:CaymanSKU:23839 - 10 mgAvailable on backorder
Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon.{41490} It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane.{41491} It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
Brand:CaymanSKU:23839 - 100 mgAvailable on backorder
Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon.{41490} It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane.{41491} It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
Brand:CaymanSKU:23839 - 25 mgAvailable on backorder
Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon.{41490} It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane.{41491} It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
Brand:CaymanSKU:23839 - 5 mgAvailable on backorder
eFT508 is a potent inhibitor of MAPK interacting protein kinases (MNK) 1 and 2 (IC50s = 50 value of <50 nM in a cellular signaling assay. eFT508 has a half-life of 5.3 hours in rats.
Brand:CaymanSKU:21957 -Out of stock
eFT508 is a potent inhibitor of MAPK interacting protein kinases (MNK) 1 and 2 (IC50s = 50 value of <50 nM in a cellular signaling assay. eFT508 has a half-life of 5.3 hours in rats.
Brand:CaymanSKU:21957 -Out of stock
eFT508 is a potent inhibitor of MAPK interacting protein kinases (MNK) 1 and 2 (IC50s = 50 value of <50 nM in a cellular signaling assay. eFT508 has a half-life of 5.3 hours in rats.
Brand:CaymanSKU:21957 -Out of stock
eFT508 is a potent inhibitor of MAPK interacting protein kinases (MNK) 1 and 2 (IC50s = 50 value of <50 nM in a cellular signaling assay. eFT508 has a half-life of 5.3 hours in rats.
Brand:CaymanSKU:21957 -Out of stock
The kinesin-like spindle protein Eg5, also known as KSP and Kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.{22151} Eg5-I is a potent inhibitor of Eg5, both in vitro and in cells (IC50s = 127 and 190 nM, respectively).{26966} It is an analog of S-trityl-L-cysteine (STLC), but is more potent and has better solubility than STLC. Eg5-I blocks bipolar spindle formation and inhibits the growth of cancer cells, with an average GI50 value of 360 nM against a broad panel of tumor cells (GI50 range = 10 nM to 3 µM).{26966} It ranges from 140- to 1200-fold more potent against cancer cells than monastrol (Item No. 15044), which also acts by inhibiting Eg5.{22151,26966}
Brand:CaymanSKU:-Out of stock
The kinesin-like spindle protein Eg5, also known as KSP and Kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.{22151} Eg5-I is a potent inhibitor of Eg5, both in vitro and in cells (IC50s = 127 and 190 nM, respectively).{26966} It is an analog of S-trityl-L-cysteine (STLC), but is more potent and has better solubility than STLC. Eg5-I blocks bipolar spindle formation and inhibits the growth of cancer cells, with an average GI50 value of 360 nM against a broad panel of tumor cells (GI50 range = 10 nM to 3 µM).{26966} It ranges from 140- to 1200-fold more potent against cancer cells than monastrol (Item No. 15044), which also acts by inhibiting Eg5.{22151,26966}
Brand:CaymanSKU:-Out of stock
The kinesin-like spindle protein Eg5, also known as KSP and Kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.{22151} Eg5-I is a potent inhibitor of Eg5, both in vitro and in cells (IC50s = 127 and 190 nM, respectively).{26966} It is an analog of S-trityl-L-cysteine (STLC), but is more potent and has better solubility than STLC. Eg5-I blocks bipolar spindle formation and inhibits the growth of cancer cells, with an average GI50 value of 360 nM against a broad panel of tumor cells (GI50 range = 10 nM to 3 µM).{26966} It ranges from 140- to 1200-fold more potent against cancer cells than monastrol (Item No. 15044), which also acts by inhibiting Eg5.{22151,26966}
Brand:CaymanSKU:-Out of stock
EGA is an inhibitor of endosomal trafficking.{46123} It increases accumulation of fluorescently labeled EGF in early endosomes in HeLa cells when used at a concentration of 20 μM. EGA inhibits cell death induced by anthrax lethal toxin in RAW264.7 cells (IC50 = 1.7 μM) as well as by additional acid-dependent bacterial toxins, including diphtheria toxin, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT), in various cell types. It also inhibits infection of Vero and HeLa cells by the low pH-dependent lymphocytic choriomeningitis (LCMV; Armstrong strain) and influenza A/WSN/33 viruses, respectively.
Brand:CaymanSKU:21882 -Out of stock
EGA is an inhibitor of endosomal trafficking.{46123} It increases accumulation of fluorescently labeled EGF in early endosomes in HeLa cells when used at a concentration of 20 μM. EGA inhibits cell death induced by anthrax lethal toxin in RAW264.7 cells (IC50 = 1.7 μM) as well as by additional acid-dependent bacterial toxins, including diphtheria toxin, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT), in various cell types. It also inhibits infection of Vero and HeLa cells by the low pH-dependent lymphocytic choriomeningitis (LCMV; Armstrong strain) and influenza A/WSN/33 viruses, respectively.
Brand:CaymanSKU:21882 -Out of stock
EGA is an inhibitor of endosomal trafficking.{46123} It increases accumulation of fluorescently labeled EGF in early endosomes in HeLa cells when used at a concentration of 20 μM. EGA inhibits cell death induced by anthrax lethal toxin in RAW264.7 cells (IC50 = 1.7 μM) as well as by additional acid-dependent bacterial toxins, including diphtheria toxin, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT), in various cell types. It also inhibits infection of Vero and HeLa cells by the low pH-dependent lymphocytic choriomeningitis (LCMV; Armstrong strain) and influenza A/WSN/33 viruses, respectively.
Brand:CaymanSKU:21882 -Out of stock
EGA is an inhibitor of endosomal trafficking.{46123} It increases accumulation of fluorescently labeled EGF in early endosomes in HeLa cells when used at a concentration of 20 μM. EGA inhibits cell death induced by anthrax lethal toxin in RAW264.7 cells (IC50 = 1.7 μM) as well as by additional acid-dependent bacterial toxins, including diphtheria toxin, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT), in various cell types. It also inhibits infection of Vero and HeLa cells by the low pH-dependent lymphocytic choriomeningitis (LCMV; Armstrong strain) and influenza A/WSN/33 viruses, respectively.
Brand:CaymanSKU:21882 -Out of stock
EGCG octaacetate is a prodrug form of (–)-epigallocatechin gallate (EGCG; Item No. 70935).{59063} It is cleaved by intracellular esterases to form EGCG. EGCG octaacetate (50 µM) reduces proteasome activity in MDA-MB-231 breast cancer cells extracts.{59064} It induces apoptosis in, and inhibits proliferation of, MDA-MB-231 cells when used at the same concentration. Dietary administration of EGCG octaacetate (0.085%) decreases colonic IL-6, IL-1β, and TNF-α levels, as well as reduces colonic shortening, tissue damage, and inflammatory cell infiltration in a mouse model of colitis induced by dextran sulfate sodium (DSS; Item No. 23250).{59065}
Brand:CaymanSKU:31144 - 10 mgAvailable on backorder
EGCG octaacetate is a prodrug form of (–)-epigallocatechin gallate (EGCG; Item No. 70935).{59063} It is cleaved by intracellular esterases to form EGCG. EGCG octaacetate (50 µM) reduces proteasome activity in MDA-MB-231 breast cancer cells extracts.{59064} It induces apoptosis in, and inhibits proliferation of, MDA-MB-231 cells when used at the same concentration. Dietary administration of EGCG octaacetate (0.085%) decreases colonic IL-6, IL-1β, and TNF-α levels, as well as reduces colonic shortening, tissue damage, and inflammatory cell infiltration in a mouse model of colitis induced by dextran sulfate sodium (DSS; Item No. 23250).{59065}
Brand:CaymanSKU:31144 - 25 mgAvailable on backorder
EGCG octaacetate is a prodrug form of (–)-epigallocatechin gallate (EGCG; Item No. 70935).{59063} It is cleaved by intracellular esterases to form EGCG. EGCG octaacetate (50 µM) reduces proteasome activity in MDA-MB-231 breast cancer cells extracts.{59064} It induces apoptosis in, and inhibits proliferation of, MDA-MB-231 cells when used at the same concentration. Dietary administration of EGCG octaacetate (0.085%) decreases colonic IL-6, IL-1β, and TNF-α levels, as well as reduces colonic shortening, tissue damage, and inflammatory cell infiltration in a mouse model of colitis induced by dextran sulfate sodium (DSS; Item No. 23250).{59065}
Brand:CaymanSKU:31144 - 50 mgAvailable on backorder
EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.{25289} It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 μM).{25289} Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.{25291,25290}
Brand:CaymanSKU:- EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.{25289} It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 μM).{25289} Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.{25291,25290}
Brand:CaymanSKU:- EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.{25289} It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 μM).{25289} Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.{25291,25290}
Brand:CaymanSKU:-
EGFR/ErbB2 inhibitor is a cell-permeable inhibitor of EGFR and c-ErbB2 (HER2, Neu; IC50s = 20 and 79 nM, respectively).{28556} It inhibits the proliferation of cancer cells overexpressing either c-ErbB2 or EGFR (IC50s = 2.3-2.5 µM).{28556} EGFR/ErbB2 inhibitor displays a high level of selectivity for these kinases.{28555}
Brand:CaymanSKU:-Available on backorder
EGFR/ErbB2 inhibitor is a cell-permeable inhibitor of EGFR and c-ErbB2 (HER2, Neu; IC50s = 20 and 79 nM, respectively).{28556} It inhibits the proliferation of cancer cells overexpressing either c-ErbB2 or EGFR (IC50s = 2.3-2.5 µM).{28556} EGFR/ErbB2 inhibitor displays a high level of selectivity for these kinases.{28555}
Brand:CaymanSKU:-Available on backorder
Type 4 cyclic nucleotide phosphodiesterase (PDE4) selectively inactivates the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP. PDE4 has been reported to play a key regulatory role in Hedgehog signaling downstream of smoothened and, thus, represents a potential therapeutic target for Hedgehog-dependent cancers.{28683} Eggmanone is a selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway.{28683} It demonstrates 40- to 50-fold lower potency at PDE3, PDE10, and PDE11 (IC50s = 3, 3.05, and 4.08 µM, respectively).{28683} Inhibition of PDE4 activity via eggmanone was shown to activate localized protein kinase A signaling, which, in turn, regulates Gli processing and translocation.{28683}
Brand:CaymanSKU:-Available on backorder
Type 4 cyclic nucleotide phosphodiesterase (PDE4) selectively inactivates the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP. PDE4 has been reported to play a key regulatory role in Hedgehog signaling downstream of smoothened and, thus, represents a potential therapeutic target for Hedgehog-dependent cancers.{28683} Eggmanone is a selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway.{28683} It demonstrates 40- to 50-fold lower potency at PDE3, PDE10, and PDE11 (IC50s = 3, 3.05, and 4.08 µM, respectively).{28683} Inhibition of PDE4 activity via eggmanone was shown to activate localized protein kinase A signaling, which, in turn, regulates Gli processing and translocation.{28683}
Brand:CaymanSKU:-Available on backorder
Type 4 cyclic nucleotide phosphodiesterase (PDE4) selectively inactivates the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP. PDE4 has been reported to play a key regulatory role in Hedgehog signaling downstream of smoothened and, thus, represents a potential therapeutic target for Hedgehog-dependent cancers.{28683} Eggmanone is a selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway.{28683} It demonstrates 40- to 50-fold lower potency at PDE3, PDE10, and PDE11 (IC50s = 3, 3.05, and 4.08 µM, respectively).{28683} Inhibition of PDE4 activity via eggmanone was shown to activate localized protein kinase A signaling, which, in turn, regulates Gli processing and translocation.{28683}
Brand:CaymanSKU:-Available on backorder
EGT-1442 is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 µM and 2 nM for human SGLT1 and SGLT2, respectively.{33505} It produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.
Brand:CaymanSKU:21359 -Out of stock
EGT-1442 is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 µM and 2 nM for human SGLT1 and SGLT2, respectively.{33505} It produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.
Brand:CaymanSKU:21359 -Out of stock
EGT-1442 is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 µM and 2 nM for human SGLT1 and SGLT2, respectively.{33505} It produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.
Brand:CaymanSKU:21359 -Out of stock
EGT-1442 is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 µM and 2 nM for human SGLT1 and SGLT2, respectively.{33505} It produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.
Brand:CaymanSKU:21359 -Out of stock
EGTA AM is a cell-permeant acetoxymethyl ester of the calcium chelator EGTA. As EGTA AM enters cells, it is hydrolyzed by intracellular esterases to produce EGTA. EGTA AM is used to evaluate the role of intracellular calcium changes in cell signaling.{31948,31949,31950}
Brand:CaymanSKU:20401 -Available on backorder
EHNA is a reversible adenosine deaminase inhibitor (IC50 = 1.2 μM in human red blood cells) that also selectively inhibits the cGMP-specific phosphodiesterase (PDE2) (IC50s = 0.8 and 2 μM from human and porcine myocardium, respectively, 3.5 μM in rat hepatocyte, and 5.5 μM in human platelet).{20010,20014} Comparatively, EHNA is much less potent at inhibiting PDE1, PDE3, or PDE4 (IC50s > 100 μM).{20010} EHNA has been used to evaluate cardioprotective and neuroprotective effects during ischemia, to study the role of cAMP/cGMP signaling, and to maintain pluripotency/prevent differentiation of human embryonic stem cells.{20013,20012,20011}
Brand:CaymanSKU:- EHNA is a reversible adenosine deaminase inhibitor (IC50 = 1.2 μM in human red blood cells) that also selectively inhibits the cGMP-specific phosphodiesterase (PDE2) (IC50s = 0.8 and 2 μM from human and porcine myocardium, respectively, 3.5 μM in rat hepatocyte, and 5.5 μM in human platelet).{20010,20014} Comparatively, EHNA is much less potent at inhibiting PDE1, PDE3, or PDE4 (IC50s > 100 μM).{20010} EHNA has been used to evaluate cardioprotective and neuroprotective effects during ischemia, to study the role of cAMP/cGMP signaling, and to maintain pluripotency/prevent differentiation of human embryonic stem cells.{20013,20012,20011}
Brand:CaymanSKU:- EHNA is a reversible adenosine deaminase inhibitor (IC50 = 1.2 μM in human red blood cells) that also selectively inhibits the cGMP-specific phosphodiesterase (PDE2) (IC50s = 0.8 and 2 μM from human and porcine myocardium, respectively, 3.5 μM in rat hepatocyte, and 5.5 μM in human platelet).{20010,20014} Comparatively, EHNA is much less potent at inhibiting PDE1, PDE3, or PDE4 (IC50s > 100 μM).{20010} EHNA has been used to evaluate cardioprotective and neuroprotective effects during ischemia, to study the role of cAMP/cGMP signaling, and to maintain pluripotency/prevent differentiation of human embryonic stem cells.{20013,20012,20011}
Brand:CaymanSKU:-
EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3.{38132} It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 μM in a Rac1 activation assay.{38131} At a concentration of 1 μM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 μM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 μM. EHop-016 (2-4 μM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis.{38134} It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (≥2.5 μM).{38133}
Brand:CaymanSKU:21557 -Out of stock
EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3.{38132} It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 μM in a Rac1 activation assay.{38131} At a concentration of 1 μM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 μM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 μM. EHop-016 (2-4 μM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis.{38134} It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (≥2.5 μM).{38133}
Brand:CaymanSKU:21557 -Out of stock
EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3.{38132} It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 μM in a Rac1 activation assay.{38131} At a concentration of 1 μM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 μM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 μM. EHop-016 (2-4 μM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis.{38134} It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (≥2.5 μM).{38133}
Brand:CaymanSKU:21557 -Out of stock
EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3.{38132} It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 μM in a Rac1 activation assay.{38131} At a concentration of 1 μM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 μM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 μM. EHop-016 (2-4 μM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis.{38134} It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (≥2.5 μM).{38133}
Brand:CaymanSKU:21557 -Out of stock
EHT 1864 is an inhibitor of the Rac subfamily of Rho GTPases, that binds to Rac1, Rac1b, Rac2, and Rac3 with Kd values of 40, 50, 50, and 250 nM, respectively.{28453} It can reverse transformation of NIH 3T3 fibroblasts caused by constitutively activated Rac1, as well as Rac-dependent transformation caused by Tiam1 or Ras.{28453} EHT 1864 inhibits APP processing by γ-secretase, reducing Αβ40 and Αβ42 accumulation.{28454} It blocks breast cancer cell invasion in a collagen matrix assay and, at 10 µM, increases the size but decreases the density of dendritic spines of hippocampal neurons in culture.{28455,28456}
Brand:CaymanSKU:-Out of stock
EHT 1864 is an inhibitor of the Rac subfamily of Rho GTPases, that binds to Rac1, Rac1b, Rac2, and Rac3 with Kd values of 40, 50, 50, and 250 nM, respectively.{28453} It can reverse transformation of NIH 3T3 fibroblasts caused by constitutively activated Rac1, as well as Rac-dependent transformation caused by Tiam1 or Ras.{28453} EHT 1864 inhibits APP processing by γ-secretase, reducing Αβ40 and Αβ42 accumulation.{28454} It blocks breast cancer cell invasion in a collagen matrix assay and, at 10 µM, increases the size but decreases the density of dendritic spines of hippocampal neurons in culture.{28455,28456}
Brand:CaymanSKU:-Out of stock
EHT 1864 is an inhibitor of the Rac subfamily of Rho GTPases, that binds to Rac1, Rac1b, Rac2, and Rac3 with Kd values of 40, 50, 50, and 250 nM, respectively.{28453} It can reverse transformation of NIH 3T3 fibroblasts caused by constitutively activated Rac1, as well as Rac-dependent transformation caused by Tiam1 or Ras.{28453} EHT 1864 inhibits APP processing by γ-secretase, reducing Αβ40 and Αβ42 accumulation.{28454} It blocks breast cancer cell invasion in a collagen matrix assay and, at 10 µM, increases the size but decreases the density of dendritic spines of hippocampal neurons in culture.{28455,28456}
Brand:CaymanSKU:-Out of stock