Cayman
Showing 11401–11550 of 45550 results
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BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay).{46495} It is selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 µM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 µM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day.
Brand:CaymanSKU:28913 - 5 mgAvailable on backorder
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).{33973} BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:19777 -Available on backorder
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).{33973} BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:19777 -Available on backorder
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).{33973} BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:19777 -Available on backorder
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).{33973} BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:19777 -Available on backorder
BAY-545 is an adenosine A2B receptor antagonist.{50105} It is selective for adenosine A2B receptors over A1, A2A, and A3 receptors with IC50 values of 66, 1,300, 820, and >6,700 nM, respectively, in CHO cell membranes expressing human recombinant receptors. BAY-545 reduces increases in the levels of IL-6 induced by the adenosine receptor agonist 5′-(N-ethylcarbamoyl)adenosine (NECA; Item No. 21420) in LL29 fibroblast cells (IC50 = 185 nM). It decreases FITC-induced increases in the levels of IL-6 in lung homogenates and cell numbers in bronchoalveolar lavage fluid (BALF) and reduces silica-induced increases in the levels of TGF-β1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis when administered at a dose of 500 mg/kg.
Brand:CaymanSKU:28420 - 1 mgAvailable on backorder
BAY-545 is an adenosine A2B receptor antagonist.{50105} It is selective for adenosine A2B receptors over A1, A2A, and A3 receptors with IC50 values of 66, 1,300, 820, and >6,700 nM, respectively, in CHO cell membranes expressing human recombinant receptors. BAY-545 reduces increases in the levels of IL-6 induced by the adenosine receptor agonist 5′-(N-ethylcarbamoyl)adenosine (NECA; Item No. 21420) in LL29 fibroblast cells (IC50 = 185 nM). It decreases FITC-induced increases in the levels of IL-6 in lung homogenates and cell numbers in bronchoalveolar lavage fluid (BALF) and reduces silica-induced increases in the levels of TGF-β1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis when administered at a dose of 500 mg/kg.
Brand:CaymanSKU:28420 - 5 mgAvailable on backorder
BAY-588 is a glucose transporter inhibitor and derivative of BAY-876 (Item No. 19961).{38214} It selectively inhibits glucose transporter 4 (Glut4), Glut1, and Glut3 over Glut2 with IC50 values of 0.5, 1.18, 5.47, and >10 μM, respectively, in CHO cells expressing human recombinant transporters.
Brand:CaymanSKU:19960 -Available on backorder
BAY-588 is a glucose transporter inhibitor and derivative of BAY-876 (Item No. 19961).{38214} It selectively inhibits glucose transporter 4 (Glut4), Glut1, and Glut3 over Glut2 with IC50 values of 0.5, 1.18, 5.47, and >10 μM, respectively, in CHO cells expressing human recombinant transporters.
Brand:CaymanSKU:19960 -Available on backorder
BAY-588 is a glucose transporter inhibitor and derivative of BAY-876 (Item No. 19961).{38214} It selectively inhibits glucose transporter 4 (Glut4), Glut1, and Glut3 over Glut2 with IC50 values of 0.5, 1.18, 5.47, and >10 μM, respectively, in CHO cells expressing human recombinant transporters.
Brand:CaymanSKU:19960 -Available on backorder
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). It is 100-fold selective for SMYD3 over other histone methyltransferases. BAY-6035 inhibits methylation of MEKK2 peptide in a cell-free assay and in cells (IC50s = 88 and 70 nM, respectively). See the Structural Genomic Consortium (SGC) website for more information.
Brand:CaymanSKU:25925 - 1 mgAvailable on backorder
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). It is 100-fold selective for SMYD3 over other histone methyltransferases. BAY-6035 inhibits methylation of MEKK2 peptide in a cell-free assay and in cells (IC50s = 88 and 70 nM, respectively). See the Structural Genomic Consortium (SGC) website for more information.
Brand:CaymanSKU:25925 - 10 mgAvailable on backorder
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). It is 100-fold selective for SMYD3 over other histone methyltransferases. BAY-6035 inhibits methylation of MEKK2 peptide in a cell-free assay and in cells (IC50s = 88 and 70 nM, respectively). See the Structural Genomic Consortium (SGC) website for more information.
Brand:CaymanSKU:25925 - 5 mgAvailable on backorder
BAY-678 is a cell permeable inhibitor of human neutrophil elastase. This product, the (R) isomer, inhibits human neutrophil elastase with an in vitro IC50 value of 20 nM.{29994,34377} BAY-678 displays greater than 2,000-fold selectivity for neutrophil elastase over a panel of 21 serine proteases, and there is no significant inhibition against 7 serine/threonine kinases and 64 pharmacologically relevant proteins.{29994,34377} It has a favorable pharmacokinetic profile and demonstrates efficacy in acute in vivo models, including protease-induced acute lung injury in mice.{29994,34377} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAY-678 is a cell permeable inhibitor of human neutrophil elastase. This product, the (R) isomer, inhibits human neutrophil elastase with an in vitro IC50 value of 20 nM.{29994,34377} BAY-678 displays greater than 2,000-fold selectivity for neutrophil elastase over a panel of 21 serine proteases, and there is no significant inhibition against 7 serine/threonine kinases and 64 pharmacologically relevant proteins.{29994,34377} It has a favorable pharmacokinetic profile and demonstrates efficacy in acute in vivo models, including protease-induced acute lung injury in mice.{29994,34377} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAY-678 is a cell permeable inhibitor of human neutrophil elastase. This product, the (R) isomer, inhibits human neutrophil elastase with an in vitro IC50 value of 20 nM.{29994,34377} BAY-678 displays greater than 2,000-fold selectivity for neutrophil elastase over a panel of 21 serine proteases, and there is no significant inhibition against 7 serine/threonine kinases and 64 pharmacologically relevant proteins.{29994,34377} It has a favorable pharmacokinetic profile and demonstrates efficacy in acute in vivo models, including protease-induced acute lung injury in mice.{29994,34377} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.{38214} It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
Brand:CaymanSKU:19961 -Available on backorder
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.{38214} It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
Brand:CaymanSKU:19961 -Available on backorder
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.{38214} It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
Brand:CaymanSKU:19961 -Available on backorder
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.{38214} It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
Brand:CaymanSKU:19961 -Available on backorder
The cysteinyl leukotrienes LTC4 and LTD4 are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G-protein coupled receptors, CysLT1 and CysLT2.{7174,8519,14081} BayCysLT2 is a potent CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively.{18564} BayCysLT2 concentration-dependently reverses LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts.{18564}
Brand:CaymanSKU:10532 - 1 mgAvailable on backorder
The cysteinyl leukotrienes LTC4 and LTD4 are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G-protein coupled receptors, CysLT1 and CysLT2.{7174,8519,14081} BayCysLT2 is a potent CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively.{18564} BayCysLT2 concentration-dependently reverses LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts.{18564}
Brand:CaymanSKU:10532 - 10 mgAvailable on backorder
The cysteinyl leukotrienes LTC4 and LTD4 are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G-protein coupled receptors, CysLT1 and CysLT2.{7174,8519,14081} BayCysLT2 is a potent CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively.{18564} BayCysLT2 concentration-dependently reverses LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts.{18564}
Brand:CaymanSKU:10532 - 25 mgAvailable on backorder
The cysteinyl leukotrienes LTC4 and LTD4 are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G-protein coupled receptors, CysLT1 and CysLT2.{7174,8519,14081} BayCysLT2 is a potent CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively.{18564} BayCysLT2 concentration-dependently reverses LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts.{18564}
Brand:CaymanSKU:10532 - 5 mgAvailable on backorder
BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death.{21319} BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.{28479} It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.{28479} BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 µM in the BAZ2A FRAP assay.{28479} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death.{21319} BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.{28479} It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.{28479} BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 µM in the BAZ2A FRAP assay.{28479} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death.{21319} BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.{28479} It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.{28479} BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 µM in the BAZ2A FRAP assay.{28479} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death.{21319} BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.{28479} It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.{28479} BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 µM in the BAZ2A FRAP assay.{28479} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.{22646}
Brand:CaymanSKU:- Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.{22646}
Brand:CaymanSKU:- Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.{22646}
Brand:CaymanSKU:- Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.{22646}
Brand:CaymanSKU:-
Bazedoxifene-d4 is intended for use as an internal standard for the quantification of bazedoxifene (Item No. 15005) by GC- or LC-MS. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.
Brand:CaymanSKU:22554 -Out of stock
Bazedoxifene-d4 is intended for use as an internal standard for the quantification of bazedoxifene (Item No. 15005) by GC- or LC-MS. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.
Brand:CaymanSKU:22554 -Out of stock
BB-22 (Item No. 14099) is an analog of the potent synthetic cannabinoid, JWH 018 (Item No. 10900) that is structurally similar to PB-22 (Item No. 14096) and its derivative, 5-fluoro PB-22 (Item No. 14095).{18291,19507} Both BB-22 and PB-22 are distinctive in that an 8-hydroxyquinoline replaces the naphthalene group of JWH 018. BB-22 3-carboxyindole metabolite is expected to be a metabolite of BB-22 that would be detectable both in serum and urine. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.
Brand:CaymanSKU:- BB-22 (Item No. 14099) is an analog of the potent synthetic cannabinoid, JWH 018 (Item No. 10900) that is structurally similar to PB-22 (Item No. 14096) and its derivative, 5-fluoro PB-22 (Item No. 14095).{18291,19507} Both BB-22 and PB-22 are distinctive in that an 8-hydroxyquinoline replaces the naphthalene group of JWH 018. BB-22 3-carboxyindole metabolite is expected to be a metabolite of BB-22 that would be detectable both in serum and urine. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.
Brand:CaymanSKU:- BB-22 (Item No. 14099) is an analog of the potent synthetic cannabinoid, JWH 018 (Item No. 10900) that is structurally similar to PB-22 (Item No. 14096) and its derivative, 5-fluoro PB-22 (Item No. 14095).{18291,19507} Both BB-22 and PB-22 are distinctive in that an 8-hydroxyquinoline replaces the naphthalene group of JWH 018. BB-22 3-carboxyindole metabolite is expected to be a metabolite of BB-22 that would be detectable both in serum and urine. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.
Brand:CaymanSKU:-
BB-Cl-Amidine is a modified version of Cl-amidine (Item No. 10599) that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide.{27726} BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.{27726} BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.
Brand:CaymanSKU:-Out of stock
BB-Cl-Amidine is a modified version of Cl-amidine (Item No. 10599) that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide.{27726} BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.{27726} BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.
Brand:CaymanSKU:-Out of stock
BB-Cl-Amidine is a modified version of Cl-amidine (Item No. 10599) that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide.{27726} BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.{27726} BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.
Brand:CaymanSKU:-Out of stock
BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-Cl-Yne inhibits PAD1-4 with Kinact/KI values of 6,400, 3,600, 10,800, and 4,900 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25378 - 1 mgAvailable on backorder
BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-Cl-Yne inhibits PAD1-4 with Kinact/KI values of 6,400, 3,600, 10,800, and 4,900 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25378 - 5 mgAvailable on backorder
BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-Cl-Yne inhibits PAD1-4 with Kinact/KI values of 6,400, 3,600, 10,800, and 4,900 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25378 - 500 µgAvailable on backorder
BB-F-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-F-Yne inhibits PAD1-4 with Kinact/KI values of 900, 1,200, 3,400, and 3,750 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25379 - 1 mgAvailable on backorder
BB-F-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-F-Yne inhibits PAD1-4 with Kinact/KI values of 900, 1,200, 3,400, and 3,750 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25379 - 5 mgAvailable on backorder
BB-F-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Item No. 17079) that contains an alkyne moiety for use in click chemistry reactions.{43084} BB-F-Yne inhibits PAD1-4 with Kinact/KI values of 900, 1,200, 3,400, and 3,750 M-1min-1, respectively. It has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
Brand:CaymanSKU:25379 - 500 µgAvailable on backorder
BC-11-38 is a potent and selective phosphodiesterase (PDE) 11 inhibitor (IC50s = 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively).{33958} Gene association studies suggested that PDE11 was involved in adrenal function, and in H295R human adrenocortical cells, BC-11-38 increased cAMP and cortisol levels and activating transcription factor 1 (ATF-1) phosphorylation.{33959,33960,33958}
Brand:CaymanSKU:20167 -Available on backorder
BC-11-38 is a potent and selective phosphodiesterase (PDE) 11 inhibitor (IC50s = 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively).{33958} Gene association studies suggested that PDE11 was involved in adrenal function, and in H295R human adrenocortical cells, BC-11-38 increased cAMP and cortisol levels and activating transcription factor 1 (ATF-1) phosphorylation.{33959,33960,33958}
Brand:CaymanSKU:20167 -Available on backorder
BC-11-38 is a potent and selective phosphodiesterase (PDE) 11 inhibitor (IC50s = 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively).{33958} Gene association studies suggested that PDE11 was involved in adrenal function, and in H295R human adrenocortical cells, BC-11-38 increased cAMP and cortisol levels and activating transcription factor 1 (ATF-1) phosphorylation.{33959,33960,33958}
Brand:CaymanSKU:20167 -Available on backorder
BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC50 = 0.9 μg/mL for Il-1β release).{38454} It decreases FBXO3 interaction with F-box/LRR-repeat protein 2 (FBXL2) in a dose-dependent manner and prevents FBXO3-dependent ubiquitination of FBXL2. It also lowers expression of Tnf receptor-associated factors (TRAFs) 1-6 without affecting TRAF1-6 mRNA levels in resting and LPS-stimulated peripheral blood mononuclear cells (PBMCs). BC-1215 (100 μg, i.p., per animal) reduces plasma levels of the inflammatory cytokines Il-6, Tnf, and Il-1β and decreases peritoneal bacteria counts in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces inflammation in mouse models of DSS-induced colitis, paw edema, and ear edema.{38455}
Brand:CaymanSKU:21964 -Out of stock
BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC50 = 0.9 μg/mL for Il-1β release).{38454} It decreases FBXO3 interaction with F-box/LRR-repeat protein 2 (FBXL2) in a dose-dependent manner and prevents FBXO3-dependent ubiquitination of FBXL2. It also lowers expression of Tnf receptor-associated factors (TRAFs) 1-6 without affecting TRAF1-6 mRNA levels in resting and LPS-stimulated peripheral blood mononuclear cells (PBMCs). BC-1215 (100 μg, i.p., per animal) reduces plasma levels of the inflammatory cytokines Il-6, Tnf, and Il-1β and decreases peritoneal bacteria counts in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces inflammation in mouse models of DSS-induced colitis, paw edema, and ear edema.{38455}
Brand:CaymanSKU:21964 -Out of stock
BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC50 = 0.9 μg/mL for Il-1β release).{38454} It decreases FBXO3 interaction with F-box/LRR-repeat protein 2 (FBXL2) in a dose-dependent manner and prevents FBXO3-dependent ubiquitination of FBXL2. It also lowers expression of Tnf receptor-associated factors (TRAFs) 1-6 without affecting TRAF1-6 mRNA levels in resting and LPS-stimulated peripheral blood mononuclear cells (PBMCs). BC-1215 (100 μg, i.p., per animal) reduces plasma levels of the inflammatory cytokines Il-6, Tnf, and Il-1β and decreases peritoneal bacteria counts in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces inflammation in mouse models of DSS-induced colitis, paw edema, and ear edema.{38455}
Brand:CaymanSKU:21964 -Out of stock
BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC50 = 0.9 μg/mL for Il-1β release).{38454} It decreases FBXO3 interaction with F-box/LRR-repeat protein 2 (FBXL2) in a dose-dependent manner and prevents FBXO3-dependent ubiquitination of FBXL2. It also lowers expression of Tnf receptor-associated factors (TRAFs) 1-6 without affecting TRAF1-6 mRNA levels in resting and LPS-stimulated peripheral blood mononuclear cells (PBMCs). BC-1215 (100 μg, i.p., per animal) reduces plasma levels of the inflammatory cytokines Il-6, Tnf, and Il-1β and decreases peritoneal bacteria counts in a mouse model of cecal ligation and puncture-induced sepsis. It also reduces inflammation in mouse models of DSS-induced colitis, paw edema, and ear edema.{38455}
Brand:CaymanSKU:21964 -Out of stock
Branched-chain amino acid transferases (BCATs) catalyze reversible transamination of leucine, isoleucine, and valine branched-chain amino acids to their respective α-keto acids, liberating L-glutamate.{20159,20160} Two forms of BCAT are present in mammals. Mitochondrial BCAT (BCATm) exists in most tissues throughout the body, whereas cytosolic BCAT (BCATc) is confined to the brain, where it regulates glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system. BCATc Inhibitor 2 is a sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM for human and rat, respectively) with 15-fold selectivity over BCATm.{27460,27458,27459} This compound has been shown to block calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and to demonstrate neuroprotective efficacy in an in vivo rat model of neurodegeneration.{27458}
Brand:CaymanSKU:9002002 - 1 mgAvailable on backorder
Branched-chain amino acid transferases (BCATs) catalyze reversible transamination of leucine, isoleucine, and valine branched-chain amino acids to their respective α-keto acids, liberating L-glutamate.{20159,20160} Two forms of BCAT are present in mammals. Mitochondrial BCAT (BCATm) exists in most tissues throughout the body, whereas cytosolic BCAT (BCATc) is confined to the brain, where it regulates glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system. BCATc Inhibitor 2 is a sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM for human and rat, respectively) with 15-fold selectivity over BCATm.{27460,27458,27459} This compound has been shown to block calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and to demonstrate neuroprotective efficacy in an in vivo rat model of neurodegeneration.{27458}
Brand:CaymanSKU:9002002 - 10 mgAvailable on backorder
Branched-chain amino acid transferases (BCATs) catalyze reversible transamination of leucine, isoleucine, and valine branched-chain amino acids to their respective α-keto acids, liberating L-glutamate.{20159,20160} Two forms of BCAT are present in mammals. Mitochondrial BCAT (BCATm) exists in most tissues throughout the body, whereas cytosolic BCAT (BCATc) is confined to the brain, where it regulates glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system. BCATc Inhibitor 2 is a sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM for human and rat, respectively) with 15-fold selectivity over BCATm.{27460,27458,27459} This compound has been shown to block calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and to demonstrate neuroprotective efficacy in an in vivo rat model of neurodegeneration.{27458}
Brand:CaymanSKU:9002002 - 5 mgAvailable on backorder
Branched-chain amino acid transferases (BCATs) catalyze reversible transamination of leucine, isoleucine, and valine branched-chain amino acids to their respective α-keto acids, liberating L-glutamate.{20159,20160} Two forms of BCAT are present in mammals. Mitochondrial BCAT (BCATm) exists in most tissues throughout the body, whereas cytosolic BCAT (BCATc) is confined to the brain, where it regulates glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system. BCATc Inhibitor 2 is a sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM for human and rat, respectively) with 15-fold selectivity over BCATm.{27460,27458,27459} This compound has been shown to block calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and to demonstrate neuroprotective efficacy in an in vivo rat model of neurodegeneration.{27458}
Brand:CaymanSKU:9002002 - 50 mgAvailable on backorder
BCECF is a fluorescent probe commonly used to measure pH.{25711} It is a dual-excitation ratiometric pH indicator with a pKa of ~6.98. Measurements of pH are made by determining the ratio of emission intensity, detected at 535 nm, when excited at 490 nm versus the emission intensity when excited at 440 nm.{25711} BCECF is membrane impermeable, whereas the acetoxymethyl ester, BCEBF-AM (Item No. 15922) is membrane permeant.
Brand:CaymanSKU:-Out of stock
BCECF is a fluorescent probe commonly used to measure pH.{25711} It is a dual-excitation ratiometric pH indicator with a pKa of ~6.98. Measurements of pH are made by determining the ratio of emission intensity, detected at 535 nm, when excited at 490 nm versus the emission intensity when excited at 440 nm.{25711} BCECF is membrane impermeable, whereas the acetoxymethyl ester, BCEBF-AM (Item No. 15922) is membrane permeant.
Brand:CaymanSKU:-Out of stock
BCECF is a fluorescent probe commonly used to measure pH.{25711} It is a dual-excitation ratiometric pH indicator with a pKa of ~6.98. Measurements of pH are made by determining the ratio of emission intensity, detected at 535 nm, when excited at 490 nm versus the emission intensity when excited at 440 nm.{25711} BCECF is membrane impermeable, whereas the acetoxymethyl ester, BCEBF-AM (Item No. 15922) is membrane permeant.
Brand:CaymanSKU:-Out of stock
BCECF AM ester is a widely-used fluorescent indicator for estimating intracellular pH.{25713,25712} This membrane-permeant compound is modified by intracellular esterases to produce BCECF, a polar fluorescein derivative that is retained by cells. Intracellular BCECF is stable and has an efflux half-life of greater than two hours.{25710} Intracellular pH measurements are made by ratio imaging, which involves determining the pH-dependent ratio of emission intensity (detected at 535 nm) when the dye is excited at 490 nm vs. the emission intensity when excited at 440 nm.{25712,25711} This approach is amenable to either spectrofluorometry or flow cytometry.{25712,25709} BCECF AM can also be used to investigate intracellular changes in other ions, including potassium.{25708}
Brand:CaymanSKU:- BCECF AM ester is a widely-used fluorescent indicator for estimating intracellular pH.{25713,25712} This membrane-permeant compound is modified by intracellular esterases to produce BCECF, a polar fluorescein derivative that is retained by cells. Intracellular BCECF is stable and has an efflux half-life of greater than two hours.{25710} Intracellular pH measurements are made by ratio imaging, which involves determining the pH-dependent ratio of emission intensity (detected at 535 nm) when the dye is excited at 490 nm vs. the emission intensity when excited at 440 nm.{25712,25711} This approach is amenable to either spectrofluorometry or flow cytometry.{25712,25709} BCECF AM can also be used to investigate intracellular changes in other ions, including potassium.{25708}
Brand:CaymanSKU:- BCECF AM ester is a widely-used fluorescent indicator for estimating intracellular pH.{25713,25712} This membrane-permeant compound is modified by intracellular esterases to produce BCECF, a polar fluorescein derivative that is retained by cells. Intracellular BCECF is stable and has an efflux half-life of greater than two hours.{25710} Intracellular pH measurements are made by ratio imaging, which involves determining the pH-dependent ratio of emission intensity (detected at 535 nm) when the dye is excited at 490 nm vs. the emission intensity when excited at 440 nm.{25712,25711} This approach is amenable to either spectrofluorometry or flow cytometry.{25712,25709} BCECF AM can also be used to investigate intracellular changes in other ions, including potassium.{25708}
Brand:CaymanSKU:-
The L-type amino acid transporters (LATs) are Na+-dependent neutral amino acid transporters.{30008} They include four members in two sub-families, with LAT1 and LAT2 belonging to solute carrier (SLC) family 7 and LAT3 and LAT4 being members of SLC43.{30008} LAT1 is overexpressed in many tumors and contributes to ribosome biogenesis and cell growth by supporting mTOR complex 1 (mTORC1) signaling.{15559} BCH is an inhibitor of LAT1 that blocks the uptake of L-leucine with an IC50 value of 131.5 µM.{30005,30007} It can inhibit all members of the LAT family at a concentration of 10 mM.{30008} In addition to eliminating the uptake of neutral amino acids, BCH suppresses mTORC1 signaling that drives DNA synthesis and cell proliferation.{30008,15559} LAT1 is also essential for the uptake of amino acid-related compounds, like L-DOPA (Item No. 13248), through the blood-brain barrier, and this can be inhibited by BCH.{30007,30006}
Brand:CaymanSKU:- The L-type amino acid transporters (LATs) are Na+-dependent neutral amino acid transporters.{30008} They include four members in two sub-families, with LAT1 and LAT2 belonging to solute carrier (SLC) family 7 and LAT3 and LAT4 being members of SLC43.{30008} LAT1 is overexpressed in many tumors and contributes to ribosome biogenesis and cell growth by supporting mTOR complex 1 (mTORC1) signaling.{15559} BCH is an inhibitor of LAT1 that blocks the uptake of L-leucine with an IC50 value of 131.5 µM.{30005,30007} It can inhibit all members of the LAT family at a concentration of 10 mM.{30008} In addition to eliminating the uptake of neutral amino acids, BCH suppresses mTORC1 signaling that drives DNA synthesis and cell proliferation.{30008,15559} LAT1 is also essential for the uptake of amino acid-related compounds, like L-DOPA (Item No. 13248), through the blood-brain barrier, and this can be inhibited by BCH.{30007,30006}
Brand:CaymanSKU:- The L-type amino acid transporters (LATs) are Na+-dependent neutral amino acid transporters.{30008} They include four members in two sub-families, with LAT1 and LAT2 belonging to solute carrier (SLC) family 7 and LAT3 and LAT4 being members of SLC43.{30008} LAT1 is overexpressed in many tumors and contributes to ribosome biogenesis and cell growth by supporting mTOR complex 1 (mTORC1) signaling.{15559} BCH is an inhibitor of LAT1 that blocks the uptake of L-leucine with an IC50 value of 131.5 µM.{30005,30007} It can inhibit all members of the LAT family at a concentration of 10 mM.{30008} In addition to eliminating the uptake of neutral amino acids, BCH suppresses mTORC1 signaling that drives DNA synthesis and cell proliferation.{30008,15559} LAT1 is also essential for the uptake of amino acid-related compounds, like L-DOPA (Item No. 13248), through the blood-brain barrier, and this can be inhibited by BCH.{30007,30006}
Brand:CaymanSKU:- The L-type amino acid transporters (LATs) are Na+-dependent neutral amino acid transporters.{30008} They include four members in two sub-families, with LAT1 and LAT2 belonging to solute carrier (SLC) family 7 and LAT3 and LAT4 being members of SLC43.{30008} LAT1 is overexpressed in many tumors and contributes to ribosome biogenesis and cell growth by supporting mTOR complex 1 (mTORC1) signaling.{15559} BCH is an inhibitor of LAT1 that blocks the uptake of L-leucine with an IC50 value of 131.5 µM.{30005,30007} It can inhibit all members of the LAT family at a concentration of 10 mM.{30008} In addition to eliminating the uptake of neutral amino acids, BCH suppresses mTORC1 signaling that drives DNA synthesis and cell proliferation.{30008,15559} LAT1 is also essential for the uptake of amino acid-related compounds, like L-DOPA (Item No. 13248), through the blood-brain barrier, and this can be inhibited by BCH.{30007,30006}
Brand:CaymanSKU:-
BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1.{48592,48593} (E/Z)-BCI (0.5-2 µM) inhibits LPS-induced expression of Dusp6 in a concentration-dependent manner and increases nuclear protein levels of Nrf2 in RAW 264.7 macrophages. It also inhibits LPS-induced increases in the production of IL-1β, IL-6, and reactive oxygen species (ROS) in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner. (E/Z)-BCI inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and induces cell death in part via the DNA damage response pathway.{48593} It reduces tumor growth in a gastric cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 35 mg/kg every seven days and has an additive effect when used in combination with CDDP (cisplatin; Item No. 13119). The (E) isomer of BCI inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 µM, respectively, for the human recombinant enzymes) and prevents pERK2 dephosphorylation induced by DUSP6 in vitro.{38246} It is selective for DUSP6 and DUSP1 over DUSP3/VHR, Cdc25B, and PTP1B, for which it has no activity. (E)-BCI induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos. This product is a mixture of the (E) and (Z) isomers of BCI.{48593}
Brand:CaymanSKU:21945 -Out of stock
BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1.{48592,48593} (E/Z)-BCI (0.5-2 µM) inhibits LPS-induced expression of Dusp6 in a concentration-dependent manner and increases nuclear protein levels of Nrf2 in RAW 264.7 macrophages. It also inhibits LPS-induced increases in the production of IL-1β, IL-6, and reactive oxygen species (ROS) in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner. (E/Z)-BCI inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and induces cell death in part via the DNA damage response pathway.{48593} It reduces tumor growth in a gastric cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 35 mg/kg every seven days and has an additive effect when used in combination with CDDP (cisplatin; Item No. 13119). The (E) isomer of BCI inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 µM, respectively, for the human recombinant enzymes) and prevents pERK2 dephosphorylation induced by DUSP6 in vitro.{38246} It is selective for DUSP6 and DUSP1 over DUSP3/VHR, Cdc25B, and PTP1B, for which it has no activity. (E)-BCI induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos. This product is a mixture of the (E) and (Z) isomers of BCI.{48593}
Brand:CaymanSKU:21945 -Out of stock
BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1.{48592,48593} (E/Z)-BCI (0.5-2 µM) inhibits LPS-induced expression of Dusp6 in a concentration-dependent manner and increases nuclear protein levels of Nrf2 in RAW 264.7 macrophages. It also inhibits LPS-induced increases in the production of IL-1β, IL-6, and reactive oxygen species (ROS) in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner. (E/Z)-BCI inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and induces cell death in part via the DNA damage response pathway.{48593} It reduces tumor growth in a gastric cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 35 mg/kg every seven days and has an additive effect when used in combination with CDDP (cisplatin; Item No. 13119). The (E) isomer of BCI inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 µM, respectively, for the human recombinant enzymes) and prevents pERK2 dephosphorylation induced by DUSP6 in vitro.{38246} It is selective for DUSP6 and DUSP1 over DUSP3/VHR, Cdc25B, and PTP1B, for which it has no activity. (E)-BCI induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos. This product is a mixture of the (E) and (Z) isomers of BCI.{48593}
Brand:CaymanSKU:21945 -Out of stock
The vanilloid receptor 1 (TRPV1) is a ligand-gated ion channel highly expressed on primary nociceptive neurons that respond to a variety of noxious stimuli, including heat, acid, and other chemical irritants. Because disruptions in TRPV1 activity cause reduced thermal nociception and hyperalgesia, this receptor is considered to be a useful target for the discovery of novel analgesics. BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.{12337,14470}
Brand:CaymanSKU:10006309 - 10 mgAvailable on backorder
The vanilloid receptor 1 (TRPV1) is a ligand-gated ion channel highly expressed on primary nociceptive neurons that respond to a variety of noxious stimuli, including heat, acid, and other chemical irritants. Because disruptions in TRPV1 activity cause reduced thermal nociception and hyperalgesia, this receptor is considered to be a useful target for the discovery of novel analgesics. BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.{12337,14470}
Brand:CaymanSKU:10006309 - 5 mgAvailable on backorder
The vanilloid receptor 1 (TRPV1) is a ligand-gated ion channel highly expressed on primary nociceptive neurons that respond to a variety of noxious stimuli, including heat, acid, and other chemical irritants. Because disruptions in TRPV1 activity cause reduced thermal nociception and hyperalgesia, this receptor is considered to be a useful target for the discovery of novel analgesics. BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.{12337,14470}
Brand:CaymanSKU:10006309 - 50 mgAvailable on backorder
BD 1008 (hydrobromide) (Item No. 9001336) is an analytical reference standard that is functionally categorized as a receptor antagonist. It is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM) that displays 4-fold selectivity for σ1 over σ2.{33110} BD 1008 is used to modulate signaling through σ receptors by cocaine and in models of learning and memory impairment.{33111,33112,33113} This product is intended for research and forensic applications.
Brand:CaymanSKU:9001336 - 1 mgAvailable on backorder
BD 1008 (hydrobromide) (Item No. 9001336) is an analytical reference standard that is functionally categorized as a receptor antagonist. It is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM) that displays 4-fold selectivity for σ1 over σ2.{33110} BD 1008 is used to modulate signaling through σ receptors by cocaine and in models of learning and memory impairment.{33111,33112,33113} This product is intended for research and forensic applications.
Brand:CaymanSKU:9001336 - 10 mgAvailable on backorder
BD 1008 (hydrobromide) (Item No. 9001336) is an analytical reference standard that is functionally categorized as a receptor antagonist. It is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM) that displays 4-fold selectivity for σ1 over σ2.{33110} BD 1008 is used to modulate signaling through σ receptors by cocaine and in models of learning and memory impairment.{33111,33112,33113} This product is intended for research and forensic applications.
Brand:CaymanSKU:9001336 - 5 mgAvailable on backorder
BD 1008 (hydrobromide) (Item No. 9001336) is an analytical reference standard that is functionally categorized as a receptor antagonist. It is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM) that displays 4-fold selectivity for σ1 over σ2.{33110} BD 1008 is used to modulate signaling through σ receptors by cocaine and in models of learning and memory impairment.{33111,33112,33113} This product is intended for research and forensic applications.
Brand:CaymanSKU:9001336 - 50 mgAvailable on backorder
BD 1047 is a selective antagonist of sigma-1 (σ1) receptors (Ki = 0.9 nM in a radioligand binding assay).{39221} It is selective for σ1 receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol (Item No. 12014) and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner.{39220} In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.{39222}
Brand:CaymanSKU:22928 - 10 mgAvailable on backorder
BD 1047 is a selective antagonist of sigma-1 (σ1) receptors (Ki = 0.9 nM in a radioligand binding assay).{39221} It is selective for σ1 receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol (Item No. 12014) and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner.{39220} In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.{39222}
Brand:CaymanSKU:22928 - 25 mgAvailable on backorder
BD 1047 is a selective antagonist of sigma-1 (σ1) receptors (Ki = 0.9 nM in a radioligand binding assay).{39221} It is selective for σ1 receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol (Item No. 12014) and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner.{39220} In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.{39222}
Brand:CaymanSKU:22928 - 5 mgAvailable on backorder
BD 1063 is an antagonist of sigma-1 (σ1) receptors (Ki = 9 nM).{39221} It is selective for σ1 receptors over σ2 (Ki = 449 nM) and serotonin 5-HT2 receptors (Ki = 2,552 nM), as well as opioid, dopamine D2, PCP, serotonin 5-HT1, α1-, α2-, and β-adrenergic receptors where it has Ki values of greater than 10 µM. BD 1063 (30 mg/kg) inhibits locomotor activity induced by cocaine (Item Nos. 16186 | ISO60176) in mice and decreases ethanol intake in a dose-dependent manner in two rat models of excessive drinking when administered at doses ranging from 3.3 to 11 mg/kg.{39221,37408}
Brand:CaymanSKU:23874 - 10 mgAvailable on backorder